2-Pyridineacetamide, 3-chloro-N-[(1R)-1-(3-chlorophenyl)ethyl]-6-[[2,2-difluoro-2-(1-oxido-2-pyridinyl)ethyl]amino]-, 1-oxide

Thrombin inhibitor 1 is a potent thrombin inhibitor (Ki=0.66 nM, 2xaPTT=0.43 μM).

Thrombin inhibitor 1 (Compound 4) is binds in the active site of thrombin with Ki of 0.66 nM, 2xaPTT=0.43 uM). Thrombin inhibitor 1 (Compound 4) is evaluated for its thrombin inhibitory potency and its functional ability to double the activated partial thromboplastin time (2xaPTT) in human plasma with a 2xaPTT of 0.43 μM[1].

[1]. Nantermet PG, et al. P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2771-5.