SR-123781A

Identification

Name
SR-123781A
Accession Number
DB05361
Description

SR-123781A is a synthetic hexadecasaccharide Factor IIa and Xa antagonist. It is under investigation by Sanofi-Aventis and Organon for the treatment of thrombosis and acute coronary syndromes (ACS).

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in cardiovascular disorders, thrombosis, and venous thromboembolism.

Contraindications & Blackbox Warnings
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Pharmacodynamics
Not Available
Mechanism of action

SR123781A is a synthetic hexadecasaccharide comprising an antithrombin (AT) binding domain, a thrombin binding domain, and a neutral methylated hexasaccharide sequence, was obtained from glucose through a convergent synthesis. SR123781A showed high affinity for human AT and was a potent catalyst of its inhibitory effect with regard to factor Xa and thrombin.

TargetActionsOrganism
UAntithrombin-IIINot AvailableHumans
UProteinase-activated receptor 1Not AvailableHumans
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
Adverse Effects
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Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Products

Categories

Drug Categories
Not Available
Classification
Not classified

Chemical Identifiers

UNII
V952P6826M
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Herbert JM, Herault JP, Bernat A, Savi P, Schaeffer P, Driguez PA, Duchaussoy P, Petitou M: SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60. [PubMed:11372679]
PubChem Substance
347910098

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory a...
Gene Name
SERPINC1
Uniprot ID
P01008
Uniprot Name
Antithrombin-III
Molecular Weight
52601.935 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Thrombin receptor activity
Specific Function
High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.
Gene Name
F2R
Uniprot ID
P25116
Uniprot Name
Proteinase-activated receptor 1
Molecular Weight
47439.83 Da

Drug created on November 18, 2007 11:24 / Updated on June 12, 2020 10:52

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