| Identification | Back Directory | [Name]
Acetamide, N-[3-[[[(1S)-4-(5-amino-2-pyridinyl)-1-[[4-(difluoromethylene)-1-piperidinyl]carbonyl]butyl]amino]sulfonyl][1,1'-biphenyl]-2-yl]- | [CAS]
363151-21-7 | [Synonyms]
SSR182289
SSR-182289
SSR182289A
SSR 182289
SSR 182289A
SSR-182289A
SSR-182289A (Free)
SSR182289A (Free),SSR 182289A (Free)
Acetamide, N-[3-[[[(1S)-4-(5-amino-2-pyridinyl)-1-[[4-(difluoromethylene)-1-piperidinyl]carbonyl]butyl]amino]sulfonyl][1,1'-biphenyl]-2-yl]- | [Molecular Formula]
C30H33F2N5O4S | [MOL File]
363151-21-7.mol | [Molecular Weight]
597.68 |
| Hazard Information | Back Directory | [Uses]
SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists [1][2]. | [IC 50]
human Thrombin: 0.031 nM (Ki); Trypsin: 54 nM (Ki); Factor VIIa/tissue factor: 167 μM (Ki); Factor IXa: >250 μM (Ki); Factor Xa: >250 μM (Ki); Plasmin: >250 μM (Ki); Urokinase: >250 μM (Ki); tPA: >250 μM (Ki); Kallikrein: >250 μM (Ki); Activated protein C: >250 μM (Ki) | [References]
[1] Jean-Michel Altenburger, et al. SSR182289A, a selective and potent orally active thrombin inhibitor. Bioorg Med Chem. 2004 Apr 1;12(7):1713-30. DOI:10.1016/j.bmc.2004.01.016
[2] Jean-Michel Altenburger, et al. SSR182289A, a selective and potent orally active thrombin inhibitor. Bioorg Med Chem. 2004 Apr 1;12(7):1713-30. DOI:10.1124/jpet.102.040667 |
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