Dabigatran产品描述：Dabigatran(BIB-953; BIBR 953ZW)是可逆的高活性直接凝血酶抑制剂（DTI），Ki为4.5 nM。
Dabigatran产品描述：Dabigatran(BIB-953; BIBR 953ZW) is a reversible ａnd selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]Target: thrombinin vitro: Dabigatran selectively ａnd reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) ａnd ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 ａnd 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 ａnd 3 mg/kg) ａnd rhesus monkeys (0.15, 0.3 ａnd 0.6 mg/kg). Dose- ａnd time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 ａnd 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 ａnd 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) ａnd fewer combined intracranial haemorrhages ａnd haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics ａnd Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1
研究领域：
Membrane Transporter/Ion Channel靶点：
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Alternative_Names:BIBR 953;BIBR 953ZW
MWt:471.51
Formula:C25H25N7O3
SMILES:N=C(N)C(C=C1)=CC=C1NCC2=NC3=CC(C(N(CCC(O)=O)C4=NC=CC=C4)=O)=CC=C3N2C
Research_Area:Cardiovascular Disease
公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、；MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足*新的科研需求；数千种产品在上海有充足备货，24-48小时内送达客户；大量产品提供免费试用装；已为全球多个知名企业、院校构建各种定制型化合物库。网址：www.medchemexpress.cn
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原创作者：MedChemExpress
