| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 2.8 nM (factor XIa), 5 nM (tryptase) | ||||||||||||
| Invitro | BMS-262084 shows more than 70-fold selectivity for human factor XIa (IC50=2.8 nM) over tryptase, trypsin, urokinase, plasma kallikrein, plasmin, yhrombin (factor IIa) and Factor IXa (IC50=0.005, 0.05, 0.542, 0.55, 1.7,10.5, and 17.4 μM, respectively)[1].BMS-262084 (1-100 μM) doubles the activated thromboplastin time in human and rat plasma at 0.14 and 2.2 μM, respectively[1]. | ||||||||||||
| 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: | ||||||||||||
| Name | BMS-262084 | ||||||||||||
| CAS | 253174-92-4 | ||||||||||||
| Formula | C18H31N7O5 | ||||||||||||
| Molar Mass | 425.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. |
BMS-262084
CAS: 253174-92-4 F: C18H31N7O5 W: 425.48
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor
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