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BMS-262084

目录号 : GC68778

BMS-262084 是一种有效,选择性和不可逆的 factor XIa 抑制剂,对人因子 XIa 的 IC50 值为 2.8 nM。BMS-262084 还抑制人类胰蛋白酶 (IC50=5 nM)。BMS-262084 具有抗血栓形成作用。

BMS-262084 Chemical Structure

Cas No.:253174-92-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥4,886.00
现货
1mg
¥2,088.00
现货
5mg
¥5,220.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

IC50: 2.8 nM (factor XIa), 5 nM (tryptase)[1]

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].

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].

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.

[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.

Chemical Properties

Cas No. 253174-92-4 SDF Download SDF
分子式 C18H31N7O5 分子量 425.48
溶解度 DMSO : 50 mg/mL (117.51 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.3503 mL 11.7514 mL 23.5029 mL
5 mM 0.4701 mL 2.3503 mL 4.7006 mL
10 mM 0.235 mL 1.1751 mL 2.3503 mL
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