| Identification | Back Directory | [Name]
L-Prolinamide, N-(methylsulfonyl)-D-phenylalanyl-N-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]- | [CAS]
162166-80-5 | [Synonyms]
BMS189664
BMS-189664
BMS 189664
BMS189664,BMS 189664
L-Prolinamide, N-(methylsulfonyl)-D-phenylalanyl-N-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]- | [Molecular Formula]
C22H34N6O4S | [MOL File]
162166-80-5.mol | [Molecular Weight]
478.61 |
| Hazard Information | Back Directory | [Uses]
BMS-189664 is a potent, selective, and orally active reversible inhibitor of a-thrombin, with an IC50 of 0.046 μM. BMS-189664 can be used for arterial and venous thrombosis research[1]. | [in vivo]
BMS-189664 is efficacious at protecting mice from thrombin-induced lethality[1].
BMS-189664 (0.2 mg/kg, iv) inhibits arterial thrombosis in cynomolgus monkey models[1].
BMS-189664 (infused at 9, 25, and 100 mg/kg/min for 1 h to achieve 0.5, 2, and 6 mg/kg) inhibits venous thrombosis in cynomolgus monkey models[1].
The oral bioavailability of BMS-189664 based on the dose-normalized AUCs after oral and iv dosing was 15 and 17% in dogs and monkeys, respectively[1].
| [References]
[1] Das J, et al. Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664. Bioorg Med Chem Lett. 2002 Jan 7;12(1):45-9. DOI:10.1016/s0960-894x(01)00667-9 |
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