363151-21-7
Chemical Structure
SSR182289
Synonym(s): SSR182289A free base
- CAS No.: 363151-21-7
- Formula:C30H33F2N5O4S
- Molecular Weight:597.68
IUPAC Name: (S)-N-(3-(N-(5-(5-aminopyridin-2-yl)-1-(4-(difluoromethylene)piperidin-1-yl)-1-oxopentan-2-yl)sulfamoyl)-[1,1'-biphenyl]-2-yl)acetamide
InChIKey: CZDGBCPZABMRBF-SANMLTNESA-N
SMILES: CC(NC1=C(S(=O)(N[C@H](C(N2CC/C(CC2)=C(F)/F)=O)CCCC3=NC=C(N)C=C3)=O)C=CC=C1C4=CC=CC=C4)=O
Biological Activity: 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].
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SSR182289 | 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 . | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
