產(chǎn)品屬性:
產(chǎn)品名稱 | 規(guī)格 | CAS號(hào) | 型號(hào) |
BIBR 953 (Dabigatran, Pradaxa) | 5mg 10mg 50mg 100mg | 211914-51-1 | EY-Y0163931 |
Cas No.211914-51-1
別名
化學(xué)名 3-[[2-[(4-carbamimidoylanilino)methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoic acid
分子式 C25H25N7O3
分子量 471.5
溶解度 <2.36 mg/mL in H2O, <2.28 mg/mL in DMSO, <2.28 mg/mL in EtOH
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
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].
References:
[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.
關(guān)鍵字: 211914-51-1;C25H25N7O3;BIBR 953 (Dabigatran;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè),公司自成立以來(lái),秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念,立足生物科技領(lǐng)域,運(yùn)用生物技術(shù)和科研試劑,發(fā)展現(xiàn)代生物科技,為各類大中小醫(yī)院及其它醫(yī)療機(jī)構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品,服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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