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BIBR-1048
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-1048图片
CAS NO:211915-06-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
BIBR-1048 (BIBR 1048) 是达比加群(一种凝血酶的直接抑制剂)的口服活性前药。
Cas No.211915-06-9
别名达比加群酯; BIBR 1048
化学名ethyl 3-[[2-[[4-[(Z)-N'-hexoxycarbonylcarbamimidoyl]anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate
Canonical SMILESCCCCCCOC(=O)N=C(C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)N
分子式C34H41N7O5
分子量627.73
溶解度≥ 30 mg/mL in DMSO, ≥ 22.13 mg/mL in EtOH
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dabigatran etexilate is a potent, selective and competitive inhibitor of thrombin. It is an oral prodrug of dabigatran. Ki=4.5 nM for human thrombin and IC50=10 nM for thrombin-induced platelet aggregation. [1] [2]

Thrombin is protein that proteolytically cleaved from coagulation factor II as the initial step in the coagulation cascade. It transforms fibrinogen into fibrin and activates other factors in function in blood homeostasis, wound healing and inflammation.

In vitro, dabigatran showed anticoagulant effects in a concentration-dependent manner. It doubled the activated partrial thromboplastin time, prothrombin time and ecarin clotting in human PPP. [1]

In rats and rhesus monkeys, activated partial throboplastin time was extended by dabigaran.

Rats orally administrated with dabigatran etexilate exerted anticoagulant effects in a dose and time –dependent manner. [1]

Compared with warfarin, dabigatran administered orally (150 mg dose) in patients with atrial fibraillation, exhibited lower rates of stroke and systemic embolism but similar rates of major hemorrhage. [2]

References:
1. Wienen W, Stassen JM, Priepke H et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.
2. Connolly SJ, Ezekowitz MD, Yusuf S et al. Dabigatran versus warfarin in patients with atrial
fibrillation. N Engl J Med. 2009 Sep 17;361(12):1139-51.