1. Metabolic Enzyme/Protease
  2. Factor XI
  3. BMS-962212 hydrochloride

BMS-962212 hydrochloride 是一种 XIa 因子 (FXIa) 抑制剂,对人源 FXIaKi 为 0.7 nM,对兔源 FXIaKi 为 3 nM。BMS-962212 hydrochloride 可阻断血栓形成同时保留正常止血功能。BMS-962212 hydrochloride 可用于血栓形成相关研究。

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BMS-962212 hydrochloride

BMS-962212 hydrochloride Chemical Structure

CAS No. : 1430115-97-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-962212 hydrochloride is a factor XIa (FXIa) inhibitor with a Ki of 0.7 nM against human FXIa and a Ki of 3 nM against rabbit FXIa. BMS-962212 hydrochloride blocks thrombosis while preserving normal hemostatic function. BMS-962212 hydrochloride is applicable to thrombosis-related research[1].

体外研究
(In Vitro)

BMS-962212 (Compound 55) (0.3 μM) hydrochloride 可使人血浆中活化部分凝血活酶时间延长 1.5 倍,表明其具有体外抗凝活性[1]
BMS-962212 hydrochloride 对 FXIa 具有高选择性,可抑制兔活化血浆激肽释放酶,其 Ki 为 1100 nM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BMS-962212 (单次推注 0.23-0.46 mg/kg;持续输注 1.55-3.1 mg/kg/h;静脉注射) hydrochloride 在 0.23 mg/kg 单次推注联合 1.55 mg/kg/h 持续输注的剂量下,可抑制兔动静脉分流血栓形成达 83%[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rabbit[1]
Dosage: 0.23 mg/kg (bolus) + 1.55 mg/kg/h (infusion); 0.46 mg/kg (bolus) + 3.1 mg/kg/h (infusion)
Administration: i.v. bolus; i.v. infusion
Result: Inhibited thrombus formation by 83%.
Increased activated partial thromboplastin time (aPTT) up to 1.8-fold over baseline.
Caused no changes in prothrombin time (PT).
Did not increase bleeding time compared to vehicle at twice the antithrombotic dose.
Resulted in bleeding times not greater than with aspirin treatment alone when combined with aspirin (4 mg/kg/h i.v.).
分子量

695.53

Formula

C32H29Cl2FN8O5

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BMS-962212 hydrochloride
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