您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > BIBR 953(Dabigatran,Pradaxa)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
BIBR 953(Dabigatran,Pradaxa)
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。
BIBR 953(Dabigatran,Pradaxa)图片
CAS NO:211914-51-1
规格:98%
分子量:471.5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Thrombin inhibitor,potent,reversible and direct
CAS:211914-51-1
分子式:C25H25N7O3
分子量:471.5
纯度:98%
存储:Store at -20°C

Background:

BIBR 953 is a potent, reversible, and direct inhibitor of thrombin with IC50 value of 9.3nM [1].


BIBR 953 shows a favorable selectivity profile and strong activity in vitro with a Ki value of 4.5nM. It also exhibits the best activity profile in vivo following administration to rats. BIBR 953 is designed to be converted into an orally active prodrug BIBR 1048 due to its highly polar, zwitterionic nature and poor oral absorption. BIBR 953 inhibits thrombin in a competitive fashion. This inhibition is rapid and reversible. BIBR 953 inhibits both clot-bound and free thrombin. BIBR 953 is demonstrated to have an anticoagulant efficacy both in vitro and ex vivo. Since thrombin can affect cell behavior and response in various tissue types via PAR signaling, BIBR 953 is found to be beneficial in many diseases including inflammation, infection, fibrosis and cancer. Clinical trials show that BIBR 953 is a highly effective anticoagulant with a good safety profile [1, 2].


参考文献:
[1] Hauel NH, Nar H, Priepke H, Ries U, Stassen JM, Wienen W. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.
[2] van Ryn J, Goss A, Hauel N, Wienen W, Priepke H, Nar H, Clemens A. The discovery of dabigatran etexilate. Front Pharmacol. 2013 Feb 12;4:12.