BMS-262084
目录号 : GC68778BMS-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。
Cas No.:253174-92-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
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.
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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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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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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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