Drugbank Logo

Showing drug card for Treprostinil (DB00374)

Legend: drug field target field enzyme field

for drugs
Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:47:39
Primary Accession Number DB00374
Secondary Accession Number
  • APRD01272
Name Treprostinil
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Treprostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. Treprostinil is marketed as Remodulin®. [Wikipedia]
Synonyms
  1. treprostinil
Brand Names
  1. Remodulin
  2. Viveta
Brand Mixtures Not Available
Chemical IUPAC Name 2-[[(2S,3S,3aR,9aR)-2-hydroxy-3-[(3R)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[g]naphthalen-8-yl]oxy]acetic acid
Chemical Formula C23H34O5
Chemical Structure Structure
CAS Registry Number 81846-19-7
InChI Identifier InChI=1/C23H34O5/c1-2-3-4-7-17(24)9-10-18-19-11-15-6-5-8-22(28-14-23(26)27)20(15)12-16(19)13-21(18)25/h5-6,8,16-19,21,24-25H,2-4,7,9-14H2,1H3,(H,26,27)/t16-,17-,18+,19-,21+/m1/s1/f/h26H
InChI Key PAJMKGZZBBTTOY-PBLAGGPHDJ
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound 54786 Link Image
PubChem Substance 192299 Link Image
ChEBI ID Not Available
PharmGKB ID PA10217 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02246552 Link Image
RxList Link http://www.rxlist.com/cgi/generic/remodulin.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Treprostinil Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 390.5131
Monoisotopic Molecular Weight 390.2406
State Solid
Melting Point Not Available
Experimental Water Solubility Insoluble at 25°C Source: PhysProp
Predicted Water Solubility 7.31e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 4.1 Source: PhysProp
Predicted LogP 3.53 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.73 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CCCCC[C@@H](O)CC[C@@H]1[C@@H](O)C[C@H]2CC3=C(C[C@@H]12)C=CC=C3OCC(O)=O
Canonical SMILES CCCCCC(O)CCC1C(O)CC2CC3=C(CC12)C=CC=C3OCC(O)=O
Drug Category
  • Antihypertensive Agents
  • Antithrombotic Agents
  • Vitamin K antagonists
ATC Codes
AHFS Codes
  • 24:12.92
Indication For use as a continuous subcutaneous infusion or intravenous infusion (for those not able to tolerate a subcutaneous infusion) for the treatment of pulmonary arterial hypertension in patients with NYHA Class II-IV symptoms to diminish symptoms associated with exercise.
Pharmacology Pulmonary arterial hypertension (PAH) is a disease in which blood pressure is abnormally high in the arteries between the heart and lungs. PAH is characterized by symptoms of shortness of breath during physical exertion. The condition can ultimately lead to heart failure. Treprostinil is a potent oral antiplatelet agent. The major pharmacologic actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. Other studies have shown that treprostinil causes a dose-related negative inotropic and lusitropic effect. No major effects on cardiac conduction have been observed.
Mechanism of Action The major pharmacological actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In addition to treprostinil's direct vasodilatory effects, it also inhibits inflammatory cytokine.
Absorption Relatively rapid and complete after subcutaneous infusion, with an absolute bioavailability approximately 100%. In patients with mild (n=4) or moderate (n=5) hepatic insufficiency and portopulmonary hypertension following a subcutaneous dose of 10 ng per kg of body weight per min for 150 mins the AUC 0-∞ was increased 3-fold and 5-fold respectively.
Toxicity Symptoms of overdose are extensions of its dose-limiting pharmacologic effects and include flushing, headache, hypotension, nausea, vomiting, and diarrhea. Most events were self-limiting and resolved with reduction or withholding of treprostinil.
Protein Binding Human plasma protein binding is approximately 91% in in vitro concentrations ranging from 330 to 10,000 µ/L.
Biotransformation Substantially metabolized by the liver, but the precise enzymes responsible are unknown. Five metabolites have been described (HU1 through HU5) however, the biological activity and metabolic fate of these are unknown. The chemical structure of HU1 is unknown. The metabolite HU5 is the glucuronide conjugate of treprostinil. The other metabolites are formed by oxidation of the 3-hydroxyoctyl side chain (HU2) and subsequent additional oxidation (HU3) or dehydration (HU4). Study results of in vitro human hepatic cytochrome P450 demonstrates that treprostinil does not inhibit CYP-1A2, 2C9, 2C19, 2D6, 2E1, or 3A. Whether treprostinil induces these enzymes has not been studied.
Half Life Terminal elimination half-life is approximately 2 to 4 hours. Plasma half-life is 34 and 85 minutes for intravenous and subcutaneous infusion of the drug, respectively.
Dosage Forms
Form Route
Solution Intravenous
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Abciximab The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Abciximab. Monitor for increased bleeding during concomitant thearpy.
Acebutolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Acenocoumarol The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Acenocoumarol. Monitor for increased bleeding during concomitant thearpy.
Acetazolamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Aliskiren Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Amiloride Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Aminosalicylic Acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Aminosalicylic acid. Monitor for increased bleeding during concomitant thearpy.
Amlodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Amyl Nitrite Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Anagrelide The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Anagrelide. Monitor for increased bleeding during concomitant thearpy.
Apraclonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Argatroban The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Argatroban. Monitor for increased bleeding during concomitant thearpy.
Aspirin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Aspirin. Monitor for increased bleeding during concomitant thearpy.
Atenolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Benazepril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bendroflumethiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Betaxolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bisoprolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bivalirudin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.
Brimonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bumetanide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Candesartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Captopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Carteolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Carvedilol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Celecoxib The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Celecoxib. Monitor for increased bleeding during concomitant thearpy.
Celiprolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Chlorothiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Chlorthalidone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Cilazapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Cilostazol The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Cilostazol. Monitor for increased bleeding during concomitant thearpy.
Citalopram The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Citalopram. Monitor for increased bleeding during concomitant thearpy.
Clevidipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Clonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Clopidogrel The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Clopidogrel. Monitor for increased bleeding during concomitant thearpy.
Cyclandelate Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Dexmedetomidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Dichlorphenamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Diclofenac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy.
Diflunisal The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diflunisal. Monitor for increased bleeding during concomitant thearpy.
Diltiazem Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Dipyridamole The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Dipyridamole. Monitor for increased bleeding during concomitant thearpy. Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Doxazosin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Drospirenone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Drotrecogin alfa The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Drotrecogin alfa. Monitor for increased bleeding during concomitant thearpy.
Enalapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Enoxaparin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Exoxaparin. Monitor for increased bleeding during concomitant thearpy.
Eplerenone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Eprosartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Eptifibatide The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Eptifibatide. Monitor for increased bleeding during concomitant thearpy.
Escitalopram The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Escitalopram. Monitor for increased bleeding during concomitant thearpy.
Esmolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ethacrynic acid Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Etodolac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Etodolac. Monitor for increased bleeding during concomitant thearpy.
Felodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Fenoprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Fenoprofen. Monitor for increased bleeding during concomitant thearpy.
Fluoxetine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluoxetine. Monitor for increased bleeding during concomitant thearpy.
Flurbiprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Flurbiprofen. Monitor for increased bleeding during concomitant thearpy.
Fluvoxamine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluvoxamine. Monitor for increased bleeding during concomitant thearpy.
Fondaparinux sodium The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Fondaparinux. Monitor for increased bleeding during concomitant thearpy.
Fosinopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Furosemide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Guanabenz Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Guanfacine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Heparin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Heparin. Monitor for increased bleeding during concomitant thearpy.
Hydralazine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Hydrochlorothiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Hydroflumethiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ibuprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ibuprofen. Monitor for increased bleeding during concomitant thearpy.
Indapamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Indomethacin The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Indomethacin. Monitor for increased bleeding during concomitant thearpy.
Irbesartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isosorbide Dinitrate Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isosorbide Mononitrate Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isradipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ketoprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketoprofen. Monitor for increased bleeding during concomitant thearpy.
Ketorolac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketorolac. Monitor for increased bleeding during concomitant thearpy.
Labetalol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Lepirudin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Lepirudin. Monitor for increased bleeding during concomitant thearpy.
Levobunolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Lisinopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Losartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Lumiracoxib The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Lumiracoxib. Monitor for increased bleeding during concomitant thearpy.
Mannitol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Meclofenamic acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meclofenamate. Monitor for increased bleeding during concomitant thearpy.
Mefenamic acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Mefenamic acid. Monitor for increased bleeding during concomitant thearpy.
Meloxicam The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meloxicam. Monitor for increased bleeding during concomitant thearpy.
Methazolamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Methyclothiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Metipranolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Metolazone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Metoprolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Minoxidil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Moexipril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nabumetone The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Nabumetone. Monitor for increased bleeding during concomitant thearpy.
Nadolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Naproxen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Naproxen. Monitor for increased bleeding during concomitant thearpy.
Nebivolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nesiritide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nicardipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nifedipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nimodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nisoldipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nitrendipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nitroglycerin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nitroprusside Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Olmesartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Oxaprozin The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Oxaprozin. Monitor for increased bleeding during concomitant thearpy.
Oxprenolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Papaverine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Paroxetine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Paroxetine. Monitor for increased bleeding during concomitant thearpy.
Penbutolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Perindopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Phenoxybenzamine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Phentolamine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Pindolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Piroxicam The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Piroxicam. Monitor for increased bleeding during concomitant thearpy.
Polythiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Polythiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Prazosin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Quinapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ramipril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Reserpine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Salsalate The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Salsalate. Monitor for increased bleeding during concomitant thearpy.
Sertraline The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Sertraline. Monitor for increased bleeding during concomitant thearpy.
Sotalol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Spironolactone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Sulindac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Sulindac. Monitor for increased bleeding during concomitant thearpy.
Telmisartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Terazosin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tiaprofenic acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tiaprofenic acid. Monitor for increased bleeding during concomitant thearpy.
Ticlopidine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Ticlopidine. Monitor for increased bleeding during concomitant thearpy.
Timolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tirofiban The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Tirofiban. Monitor for increased bleeding during concomitant thearpy.
Tizanidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tolazoline Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tolmetin The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tolmetin. Monitor for increased bleeding during concomitant thearpy.
Torasemide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Trandolapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Triamterene Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Trichlormethiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Urea Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Valsartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Verapamil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Warfarin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Warfarin. Monitor for increased bleeding during concomitant thearpy.
rivaroxaban The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Rivaroxaban. Monitor for increased bleeding during concomitant thearpy.
Food Interactions Not Available
Pathways Not Available
General References
  1. Wikipedia Link Image
  2. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. P2Y purinoceptor 12
  2. Small inducible cytokine A23
  3. Peroxisome proliferator-activated receptor delta
Drug Target 1 [top]
Target 1 ID 122
Target 1 Name P2Y purinoceptor 12
Target 1 Synonyms
  1. ADP-glucose receptor
  2. ADPG-R
  3. P2T(AC)
  4. P2Y(AC)
  5. P2Y(ADP)
  6. P2Y(cyc)
  7. P2Y12
  8. P2Y12 platelet ADP receptor
  9. SP1999
Target 1 Gene Name P2RY12
Target 1 Protein Sequence >P2Y purinoceptor 12 
MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI
IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI
DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS
EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI
IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF
LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
Target 1 Number of Residues 347
Target 1 Molecular Weight 39439
Target 1 Theoretical pI 9.99
Target 1 GO Classification
Function
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Involved in platelets aggregation
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 26-46
  • 59-79
  • 100-120
  • 143-163
  • 192-212
  • 234-254
  • 282-302
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 12083902 Link Image
Target 1 UniProtKB/Swiss-Prot ID Q9H244 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name P2Y12_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1029 bp 
ATGCAAGCCGTCGACAACCTCACCTCTGCGCCTGGGAACACCAGTCTGTGCACCAGAGAC
TACAAAATCACCCAGGTCCTCTTCCCACTGCTCTACACTGTCCTGTTTTTTGTTGGACTT
ATCACAAATGGCCTGGCGATGAGGATTTTCTTTCAAATCCGGAGTAAATCAAACTTTATT
ATTTTTCTTAAGAACACAGTCATTTCTGATCTTCTCATGATTCTGACTTTTCCATTCAAA
ATTCTTAGTGATGCCAAACTGGGAACAGGACCACTGAGAACTTTTGTGTGTCAAGTTACC
TCCGTCATATTTTATTTCACAATGTATATCAGTATTTCATTCCTGGGACTGATAACTATC
GATCGCTACCAGAAGACCACCAGGCCATTTAAAACATCCAACCCCAAAAATCTCTTGGGG
GCTAAGATTCTCTCTGTTGTCATCTGGGCATTCATGTTCTTACTCTCTTTGCCTAACATG
ATTCTGACCAACAGGCAGCCGAGAGACAAGAATGTGAAGAAATGCTCTTTCCTTAAATCA
GAGTTCGGTCTAGTCTGGCATGAAATAGTAAATTACATCTGTCAAGTCATTTTCTGGATT
AATTTCTTAATTGTTATTGTATGTTATACACTCATTACAAAAGAACTGTACCGGTCATAC
GTAAGAACGAGGGGTGTAGGTAAAGTCCCCAGGAAAAAGGTGAACGTCAAAGTTTTCATT
ATCATTGCTGTATTCTTTATTTGTTTTGTTCCTTTCCATTTTGCCCGAATTCCTTACACC
CTGAGCCAAACCCGGGATGTCTTTGACTGCACTGCTGAAAATACTCTGTTCTATGTGAAA
GAGAGCACTCTGTGGTTAACTTCCTTAAATGCATGCCTGGATCCGTTCATCTATTTTTTC
CTTTGCAAGTCCTTCAGAAATTCCTTGATAAGTATGCTGAAGTGCCCCAATTCTGCAACA
TCTCTGTCCCAGGACAATAGGAAAAAAGAACAGGATGGTGGTGACCCAAATGAAGAGACT
CCAATGTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID P2RY12 Link Image
Target 1 GenAtlas ID P2RY12 Link Image
Target 1 HGNC ID HGNC:18124 Link Image
Target 1 Chromosome Location 3
Target 1 Locus 3q24-q25
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Zhang FL, Luo L, Gustafson E, Lachowicz J, Smith M, Qiao X, Liu YH, Chen G, Pramanik B, Laz TM, Palmer K, Bayne M, Monsma FJ Jr: ADP is the cognate ligand for the orphan G protein-coupled receptor SP1999. J Biol Chem. 2001 Mar 16;276(11):8608-15. Epub 2000 Dec 4. [PubMed Link Image]
  2. Hollopeter G, Jantzen HM, Vincent D, Li G, England L, Ramakrishnan V, Yang RB, Nurden P, Nurden A, Julius D, Conley PB: Identification of the platelet ADP receptor targeted by antithrombotic drugs. Nature. 2001 Jan 11;409(6817):202-7. [PubMed Link Image]
  3. Takasaki J, Kamohara M, Saito T, Matsumoto M, Matsumoto S, Ohishi T, Soga T, Matsushime H, Furuichi K: Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor. Mol Pharmacol. 2001 Sep;60(3):432-9. [PubMed Link Image]
  4. Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S: Identification of G protein-coupled receptor genes from the human genome sequence. FEBS Lett. 2002 Jun 5;520(1-3):97-101. [PubMed Link Image]
Target 1 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 562
Target 2 Name Small inducible cytokine A23
Target 2 Synonyms
  1. CCL23
  2. CK-beta-8
  3. CKB-8
  4. MIP-3
  5. MPIF-1
  6. Macrophage inflammatory protein 3
  7. Myeloid progenitor inhibitory factor 1
  8. Small inducible cytokine A23 precursor
Target 2 Gene Name CCL23
Target 2 Protein Sequence >Small inducible cytokine A23 precursor 
MKVSVAALSCLMLVTALGSQARVTKDAETEFMMSKLPLENPVLLDRFHATSADCCISYTP
RSIPCSLLESYFETNSECSKPGVIFLTKKGRRFCANPSDKQVQVCMRMLKLDTRIKTRKN
Target 2 Number of Residues 122
Target 2 Molecular Weight 13443
Target 2 Theoretical pI 9.17
Target 2 GO Classification
Function
signal transducer activity
receptor binding
cytokine activity
chemokine activity
Process
response to stimulus
response to biotic stimulus
defense response
immune response
Component
extracellular region
Target 2 General Function Involved in chemokine activity
Target 2 Specific Function Shows chemotactic activity for monocytes, resting T- lymphocytes, and neutrophils, but not for activated lymphocytes. Inhibits proliferation of myeloid progenitor cells in colony formation assays. This protein can bind heparin. Binds CCR1. CCL23(19-99), CCL23(22-99), CCL23(27-99), CCL23(30-99) are more potent chemoattractants than the small inducible cytokine A23
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-21
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 1916250 Link Image
Target 2 UniProtKB/Swiss-Prot ID P55773 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name CCL23_HUMAN Link Image
Target 2 PDB ID 1G91 Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Secreted protein
Target 2 Gene Sequence >363 bp 
ATGAAGGTCTCCGTGGCTGCCCTCTCCTGCCTCATGCTTGTTACTGCCCTTGGATCCCAG
GCCCGGGTCACAAAAGATGCAGAGACAGAGTTCATGATGTCAAAGCTTCCATTGGAAAAT
CCAGTACTTCTGGACAGATTCCATGCTACTAGTGCTGACTGCTGCATCTCCTACACCCCA
CGAAGCATCCCGTGTTCACTCCTGGAGAGTTACTTTGAAACGAACAGCGAGTGCTCCAAG
CCGGGTGTCATCTTCCTCACCAAGAAGGGGCGACGTTTCTGTGCCAACCCCAGTGATAAG
CAAGTTCAGGTTTGCATGAGAATGCTGAAGCTGGACACACGGATCAAGACCAGGAAGAAT
TGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID CCL23 Link Image
Target 2 GenAtlas ID CCL23 Link Image
Target 2 HGNC ID HGNC:10622 Link Image
Target 2 Chromosome Location 17
Target 2 Locus 17q12
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Nomiyama H, Fukuda S, Iio M, Tanase S, Miura R, Yoshie O: Organization of the chemokine gene cluster on human chromosome 17q11.2 containing the genes for CC chemokine MPIF-1, HCC-2, HCC-1, LEC, and RANTES. J Interferon Cytokine Res. 1999 Mar;19(3):227-34. [PubMed Link Image]
  2. Rajarathnam K, Li Y, Rohrer T, Gentz R: Solution structure and dynamics of myeloid progenitor inhibitory factor-1 (MPIF-1), a novel monomeric CC chemokine. J Biol Chem. 2001 Feb 16;276(7):4909-16. Epub 2000 Nov 1. [PubMed Link Image]
  3. Patel VP, Kreider BL, Li Y, Li H, Leung K, Salcedo T, Nardelli B, Pippalla V, Gentz S, Thotakura R, Parmelee D, Gentz R, Garotta G: Molecular and functional characterization of two novel human C-C chemokines as inhibitors of two distinct classes of myeloid progenitors. J Exp Med. 1997 Apr 7;185(7):1163-72. [PubMed Link Image]
  4. Wells TN, Peitsch MC: The chemokine information source: identification and characterization of novel chemokines using the WorldWideWeb and expressed sequence tag databases. J Leukoc Biol. 1997 May;61(5):545-50. [PubMed Link Image]
  5. Youn BS, Zhang SM, Broxmeyer HE, Cooper S, Antol K, Fraser M Jr, Kwon BS: Characterization of CKbeta8 and CKbeta8-1: two alternatively spliced forms of human beta-chemokine, chemoattractants for neutrophils, monocytes, and lymphocytes, and potent agonists at CC chemokine receptor 1. Blood. 1998 May 1;91(9):3118-26. [PubMed Link Image]
Target 2 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 1502
Target 3 Name Peroxisome proliferator-activated receptor delta
Target 3 Synonyms
  1. NUC1
  2. NUCI
  3. Nuclear hormone receptor 1
  4. PPAR- beta
  5. PPAR-delta
Target 3 Gene Name PPARD
Target 3 Protein Sequence >Peroxisome proliferator-activated receptor delta 
MEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQM
GCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKK
NRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSK
HIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKE
ISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNK
DGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGD
RPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRI
KKTETETSLHPLLQEIYKDMY
Target 3 Number of Residues 448
Target 3 Molecular Weight 49904
Target 3 Theoretical pI 7.65
Target 3 GO Classification
Function
steroid hormone receptor activity
transcription factor activity
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
binding
nucleic acid binding
DNA binding
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 3 General Function Involved in DNA binding
Target 3 Specific Function Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Decreases expression of NPC1L1 once activated by a ligand
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • None
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 190230 Link Image
Target 3 UniProtKB/Swiss-Prot ID Q03181 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name PPARD_HUMAN Link Image
Target 3 PDB ID 1Y0S Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Nucleus
Target 3 Gene Sequence >1326 bp 
ATGGAGCAGCCACAGGAGGAAGCCCCTGAGGTCCGGGAAGAGGAGGAGAAAGAGGAAGTG
GCAGAGGCAGAAGGAGCCCCAGAGCTCAATGGGGGACCACAGCATGCACTTCCTTCCAGC
AGCTACACAGACCTCTCCCGGAGCTCCTCGCCACCCTCACTGCTGGACCAACTGCAGATG
GGCTGTGACGGGGCCTCATGCGGCAGCCTCAACATGGAGTGCCGGGTGTGCGGGGACAAG
GCATCGGGCTTCCACTACGGTGTTCATGCATGTGAGGGGTGCAAGGGCTTCTTCCGTCGT
ACGATCCGCATGAAGCTGGAGTACGAGAAGTGTGAGCGCAGCTGCAAGATTCAGAAGAAG
AACCGCAACAAGTGCCAGTACTGCCGCTTCCAGAAGTGCCTGGCACTGGGCATGTCACAC
AACGCTATCCGTTTTGGTCGGATGCCGGAGGCTGAGAAGAGGAAGCTGGTGGCAGGGCTG
ACTGCAAACGAGGGGAGCCAGTACAACCCACAGGTGGCCGACCTGAAGGCCTTCTCCAAG
CACATCTACAATGCCTACCTGAAAAACTTCAACATGACCAAAAAGAAGGCCCGCAGCATC
CTCACCGGCAAAGCCAGCCACACGGCGCCCTTTGTGATCCACGACATCGAGACATTGTGG
CAGGCAGAGAAGGGGCTGGTGTGGAAGCAGTTGGTGAATGGCCTGCCTCCCTACAAGGAG
ATCAGCGTGCACGTCTTCTACCGCTGCCAGTGCACCACAGTGGAGACCGTGCGGGAGCTC
ACTGAGTTCGCCAAGAGCATCCCCAGCTTCAGCAGCCTCTTCCTCAACGACCAGGTTACC
CTTCTCAAGTATGGCGTGCACGAGGCCATCTTCGCCATGCTGGCCTCTATCGTCAACAAG
GACGGGCTGCTGGTAGCCAACGGCAGTGGCTTTGTCACCCGTGAGTTCCTGCGCAGCCTC
CGCAAACCCTTCAGTGATATCATTGAGCCTAAGTTTGAATTTGCTGTCAAGTTCAACGCC
CTGGAACTTGATGACAGTGACCTGGCCCTATTCATTGCGGCCATCATTCTGTGTGGAGAC
CGGCCAGGCCTCATGAACGTTCCACGGGTGGAGGCTATCCAGGACACCATCCTGCGTGCC
CTCGAATTCCACCTGCAGGCCAACCACCCTGATGCCCAGTACCTCTTCCCCAAGCTGCTG
CAGAAGATGGCTGACCTGCGGCAACTGGTCACCGAGCACGCCCAGATGATGCAGCGGATC
AAGAAGACCGAAACCGAGACCTCGCTGCACCCTCTGCTCCAGGAGATCTACAAGGACATG
TACTAA
Target 3 GenBank Gene ID
Target 3 GeneCard ID PPARD Link Image
Target 3 GenAtlas ID PPARD Link Image
Target 3 HGNC ID HGNC:9235 Link Image
Target 3 Chromosome Location 6
Target 3 Locus 6p21.2-p21.1
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Skogsberg J, Kannisto K, Roshani L, Gagne E, Hamsten A, Larsson C, Ehrenborg E: Characterization of the human peroxisome proliferator activated receptor delta gene and its expression. Int J Mol Med. 2000 Jul;6(1):73-81. [PubMed Link Image]
  2. Schmidt A, Endo N, Rutledge SJ, Vogel R, Shinar D, Rodan GA: Identification of a new member of the steroid hormone receptor superfamily that is activated by a peroxisome proliferator and fatty acids. Mol Endocrinol. 1992 Oct;6(10):1634-41. [PubMed Link Image]
  3. Mungall AJ, Palmer SA, Sims SK, Edwards CA, Ashurst JL, Wilming L, Jones MC, Horton R, Hunt SE, Scott CE, Gilbert JG, Clamp ME, Bethel G, Milne S, Ainscough R, Almeida JP, Ambrose KD, Andrews TD, Ashwell RI, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Barker DJ, Barlow KF, Bates K, Beare DM, Beasley H, Beasley O, Bird CP, Blakey S, Bray-Allen S, Brook J, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Carder C, Carter NP, Chapman JC, Clark SY, Clark G, Clee CM, Clegg S, Cobley V, Collier RE, Collins JE, Colman LK, Corby NR, Coville GJ, Culley KM, Dhami P, Davies J, Dunn M, Earthrowl ME, Ellington AE, Evans KA, Faulkner L, Francis MD, Frankish A, Frankland J, French L, Garner P, Garnett J, Ghori MJ, Gilby LM, Gillson CJ, Glithero RJ, Grafham DV, Grant M, Gribble S, Griffiths C, Griffiths M, Hall R, Halls KS, Hammond S, Harley JL, Hart EA, Heath PD, Heathcott R, Holmes SJ, Howden PJ, Howe KL, Howell GR, Huckle E, Humphray SJ, Humphries MD, Hunt AR, Johnson CM, Joy AA, Kay M, Keenan SJ, Kimberley AM, King A, Laird GK, Langford C, Lawlor S, Leongamornlert DA, Leversha M, Lloyd CR, Lloyd DM, Loveland JE, Lovell J, Martin S, Mashreghi-Mohammadi M, Maslen GL, Matthews L, McCann OT, McLaren SJ, McLay K, McMurray A, Moore MJ, Mullikin JC, Niblett D, Nickerson T, Novik KL, Oliver K, Overton-Larty EK, Parker A, Patel R, Pearce AV, Peck AI, Phillimore B, Phillips S, Plumb RW, Porter KM, Ramsey Y, Ranby SA, Rice CM, Ross MT, Searle SM, Sehra HK, Sheridan E, Skuce CD, Smith S, Smith M, Spraggon L, Squares SL, Steward CA, Sycamore N, Tamlyn-Hall G, Tester J, Theaker AJ, Thomas DW, Thorpe A, Tracey A, Tromans A, Tubby B, Wall M, Wallis JM, West AP, White SS, Whitehead SL, Whittaker H, Wild A, Willey DJ, Wilmer TE, Wood JM, Wray PW, Wyatt JC, Young L, Younger RM, Bentley DR, Coulson A, Durbin R, Hubbard T, Sulston JE, Dunham I, Rogers J, Beck S: The DNA sequence and analysis of human chromosome 6. Nature. 2003 Oct 23;425(6960):805-11. [PubMed Link Image]
Target 3 Drug References
  1. Ali FY, Egan K, FitzGerald GA, Desvergne B, Wahli W, Bishop-Bailey D, Warner TD, Mitchell JA: Role of prostacyclin versus peroxisome proliferator-activated receptor beta receptors in prostacyclin sensing by lung fibroblasts. Am J Respir Cell Mol Biol. 2006 Feb;34(2):242-6. Epub 2005 Oct 20. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.