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Betrixaban
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。
Betrixaban图片
CAS NO:330942-05-7
规格:98%
分子量:451.91
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Factor Xa inhibitor
CAS:330942-05-7
分子式:C23H22ClN5O3
分子量:451.91
纯度:98%
存储:Store at -20°C

Background:

Betrixaban is a highly potent, selective, and orally efficacious inhibitor of factor Xa with IC50 value of 1.5nM [1].


Betrixaban shows excellent anticoagulant potency in vitro. In the rabbit deep vein thrombosis model, the concentration of betrixaban required to double the rabbit prothrombin time is below 2μM. Betrixaban is selective for fXa and has poor activity for thrombin, trypsin, t-PA and aPC. The patch clamp hERG assay shows that betrixaban has low affinity with hERG suggesting it is safer than other candidate compounds. In addition, betrixaban displays a profile of good oral bioavailability and oral exposure, long half-life in animal models. It has bioavailability of 51.6% at dose of 0.5 mg/kg IV and 2.5 mg/kg PO. Furthermore, the Phase II study has proved betrixaban as an oral fXa inhibitor for prevention of venous thromboembolic events [1].


参考文献:
[1] Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85.