Identification

Name
SLx-4090
Accession Number
DB05678
Type
Small Molecule
Groups
Investigational
Description

SLx-4090 is a microsomal triglyceride transfer protein (MTTP) inhibitor potentially for the treatment of type 2 diabetes. [1]

Structure
Thumb
Synonyms
Not Available
External IDs
KD-026 / KD026 / SLx 4090 / SLx-4090 / SLx4090
Categories
UNII
F84YQX13FV
CAS number
913541-47-6
Weight
Average: 546.546
Monoisotopic: 546.176641782
Chemical Formula
C31H25F3N2O4
InChI Key
AZUIUVJESCFSLJ-UHFFFAOYSA-N
InChI
InChI=1S/C31H25F3N2O4/c1-39-27-9-5-8-26(28(27)20-10-13-23(14-11-20)31(32,33)34)29(37)35-24-15-12-22-19-36(17-16-21(22)18-24)30(38)40-25-6-3-2-4-7-25/h2-15,18H,16-17,19H2,1H3,(H,35,37)
IUPAC Name
6-methoxy-N-[2-(phenoxycarbonyl)-1,2,3,4-tetrahydroisoquinolin-6-yl]-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboximidic acid
SMILES
COC1=CC=CC(C(O)=NC2=CC=C3CN(CCC3=C2)C(=O)OC2=CC=CC=C2)=C1C1=CC=C(C=C1)C(F)(F)F

Pharmacology

Indication

Investigated for use/treatment in hyperlipidemia.

Pharmacodynamics
Not Available
Mechanism of action

SLx-4090 inhibits Microsomal Triglyceride Transfer Protein (MTP). It acts selectively in the enterocytes lining the gastrointestinal tract, preventing the formation of chylomicrons which are used to transport triglyceride (TG) and cholesterol into the systemic circulation.

TargetActionsOrganism
UMicrosomal triglyceride transfer protein large subunit
inhibitor
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Kim E, Campbell S, Schueller O, Wong E, Cole B, Kuo J, Ellis J, Ferkany J, Sweetnam P: A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85. doi: 10.1124/jpet.110.177527. Epub 2011 Mar 15. [PubMed:21406547]
External Links
ChemSpider
58540436

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentHyperlipidemias1
2CompletedTreatmentHypertriglyceridemias1
2CompletedTreatmentType 2 Diabetes Mellitus2
2RecruitingTreatmentType 1 Hyperlipoproteinemia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000311 mg/mLALOGPS
logP5.72ALOGPS
logP7.65ChemAxon
logS-6.2ALOGPS
pKa (Strongest Acidic)4.71ChemAxon
pKa (Strongest Basic)0.84ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area71.36 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity147.44 m3·mol-1ChemAxon
Polarizability54.55 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Protein heterodimerization activity
Specific Function
Catalyzes the transport of triglyceride, cholesteryl ester, and phospholipid between phospholipid surfaces (PubMed:23475612, PubMed:8939939, PubMed:26224785, PubMed:25108285, PubMed:22236406). Requ...
Gene Name
MTTP
Uniprot ID
P55157
Uniprot Name
Microsomal triglyceride transfer protein large subunit
Molecular Weight
99350.255 Da
References
  1. Kim E, Campbell S, Schueller O, Wong E, Cole B, Kuo J, Ellis J, Ferkany J, Sweetnam P: A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85. doi: 10.1124/jpet.110.177527. Epub 2011 Mar 15. [PubMed:21406547]

Drug created on November 18, 2007 11:26 / Updated on November 02, 2018 06:11