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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Factor Xa-Asundexian
Asundexian

Chemical Structure : Asundexian

CAS No.: 2064121-65-7

Asundexian (BAY 2433334, BAY2433334)

货号: PC-73137Not For Human Use, Lab Use Only.

Asundexian (BAY 2433334) is a highly potent, selective and orally active inhibitor of Factor XIa (FXIa) with IC50 of 0.92 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Asundexian (BAY 2433334) is a highly potent, selective and orally active inhibitor of Factor XIa (FXIa) with IC50 of 0.92 nM.
Asundexian (BAY 2433334) shows favorable selectivity of greater than 1000-fold versus serine proteases associated with the hemostatic system, including FVIIa, FIXa, FXa, FXIIa, thrombin, urokinase, tissue plasminogen activator, activated protein C.
Asundexian (BAY 2433334) prolongs the clotting time in the aPTT assay in human plasma with EC50 of 0.2 uM.
Asundexian (BAY 2433334) reduces FXIa activity, thrombin generation triggered by contact activation or low concentrations of tissue factor, and prolongs activated partial thromboplastin time in human, rabbit and various other species, but not in rodents.
Asundexian (BAY 2433334) reduces thrombus weight in the FeCl2 -injury models.
Asundexian (BAY 2433334) reduces thrombus weight when administered before or during thrombus formation in the AV-shunt model.

物理化学性质&存储条件

分子量 592.936
分子式 C26H21ClF4N6O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

100 mM in DMSO (59.3 mg/mL)

Chemical Name/SMILES

(S)-4-(2-(4-(5-chloro-2-(4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl)phenyl)-5-methoxy-2-oxopyridin-1(2H)-yl)butanamido)-2-fluorobenzamide

参考文献

1. Stefan Heitmeier, et al. J Thromb Haemost. 2022 Mar 15. doi: 10.1111/jth.15700.
2. Susanne Roehrig, et al. Journal of Medicinal Chemistry September 5, 2023.

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