Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C12H21N3O2 |
Molecular Weight | 239.314 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCN1C=NC(C[C@H](CCCN)C(O)=O)=C1
InChI
InChIKey=OTDGPKRCQXSTPV-JTQLQIEISA-N
InChI=1S/C12H21N3O2/c1-2-6-15-8-11(14-9-15)7-10(12(16)17)4-3-5-13/h8-10H,2-7,13H2,1H3,(H,16,17)/t10-/m0/s1
Pfizer was developing UK-396,082, an imidazole-propionic acid, as an oral treatment for thrombosis and pulmonary fibrosis. UK-396,082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI; TAFIa) with Ki of 10 nM. UK-396,082 displays excellent selectivity over plasma carboxypeptidase N (>1,000-fold); exhibits antithrombotic efficacy in a rabbit model of venous thrombosis, yet has no effect on surgical bleeding in the rabbit; possesses excellent preclinical and clinical pharmacokinetic profile. UK-396,082 showed potential for the treatment of thrombosis and other fibrin-dependent diseases in humans, however its development was discontinued.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01091532
100 - 1000 mg given orally twice daily for 14 days.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17990866
UK-396,082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI; TAFIa) with Ki of 10 nM.
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SUBSTANCE RECORD