2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. BMS-654457

BMS-654457是 (FXIa) 的小分子可逆抑制剂，与人和兔FXIa结合的Ki 值分别为 0.2 和 0.42 nM。

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BMS-654457 Chemical Structure

BMS-654457 Chemical Structure

CAS No. : 1004551-41-0

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BMS-654457 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.

体外研究
(In Vitro)

BMS-654457 shows comparable in vitro potency against FXIa in humans (Ki=0.2 nM) and in rabbits (Ki =0.42 nM), and was over 500-fold selective against coagulation-related proteases (thrombin, FXa and FVIIa) in these species[1].

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

BMS-654457 相关抗体:
体内研究
(In Vivo)

BMS-654457 is effective in the prevention of arterial thrombosis in rabbits with limited effects on bleeding time. BMS-654457 is a promising antithrombotic therapy with a wide therapeutic window[1].

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

603.71

Formula

C36H37N5O4
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
Cell Assay

Platelet aggregation is measured in hirudin-treated rabbit platelet-rich plasma (PRP) with a platelet aggregometer. PRP is mixed with 2.5 μL of vehicle or BMS-654457 at 1 and 10 μM and incubated for 2 min at 37°C. Peak platelet aggregation is determined after the addition of 2.5 μL of the agonist (ADP at 10 μM, arachidonic acid at 250 μM and collagen at 10 μg/mL, final concentration)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rabbits[1]

[1]BMS-654457 or vehicle (10 % N-N-dimethylacetamide:90 % of 5 % dextrose) is administered as a bolus plus sustaining IV infusion begun 30 min prior to each protocol. Treatment groups include BMS-654457 (mg/kg+mg/kg/h) at 0.011+0.008, 0.037+0.027, 0.11+0.08, 0.37+0.27 and 1.1 +0.8 or vehicle (n=6 per group). The plasma concentration that increased iCBF to EC50 was estimated for BMS654457[1].

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

BMS-654457 相关分类

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  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

BMS-6544571004551-41-0BMS654457BMS 654457Factor XaFxaInhibitorinhibitorinhibit

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产品名称：
BMS-654457
目录号：
HY-12631
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