| Identification | Back Directory | [Name]
BMS-262084 | [CAS]
253174-92-4 | [Synonyms]
BMS-262084
I0IR71971G
CHEMBL71037
UNII-I0IR71971G | [Molecular Formula]
C18H31N7O5 | [MDL Number]
MFCD34567230 | [MOL File]
253174-92-4.mol | [Molecular Weight]
425.48 |
| Hazard Information | Back Directory | [Uses]
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects[1][2]. | [in vivo]
BMS-262084 (2-12 mg/kg + 2-12 mg/kg/h; i.v.) reduces carotid artery thrombus weight and improves both vessel patency and integrated flow in rats[1].
| Animal Model: | Male Sprague Dawley rats (310-390 g) were induced venous thrombosis by FeCl2[1] | | Dosage: | 2 mg/kg + 2 mg/kg/h, 6 mg/kg + 6 mg/kg/h, 12 mg/kg + 12 mg/kg/h | | Administration: | I.v. 10 min before FeCl2 application | | Result: | Reduced carotid artery thrombus weight by 73% at the dose of 12 mg/kg + 12 mg/kg/h.
Improved both vessel patency and integrated flow. |
| [References]
[1] Schumacher WA, et, al. Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats. Eur J Pharmacol. 2007 Sep 10;570(1-3):167-74. DOI:10.1016/j.ejphar.2007.05.043
[2] Qian X, et, al. A stereoselective synthesis of BMS-262084, an azetidinone-based tryptase inhibitor. J Org Chem. 2002 May 31;67(11):3595-600. DOI:10.1021/jo010757o |
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