BMS-262084

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BMS-262084

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

253174-92-4

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。

生物活性

BMS-262084 is a potent, selective and irreversible inhibitor offactor XIa, with anIC₅₀of 2.8 nM against human factor XIa. BMS-262084 also inhibits humantryptase(IC₅₀=5 nM). BMS-262084 exhibits antithrombotic effects^[1]^[2].

IC₅₀& Target

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

体外研究
(In Vitro)

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].

体内研究
(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 FeCl₂application
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.

分子量

425.48

Formula

C₁₈H₃₁N₇O₅

CAS 号

253174-92-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.