BIBR 953(Dabigatran)

产品编号: DCAPI1112 Featured
BIBR 953(Dabigatran)
结构式
211914-51-1
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中国地区超过5000个高品质化合物库存
应用领域
Dabigatran (BIBR 953),口服抗凝剂,是可逆的,竞争性的直接凝血酶 (thrombin) 抑制剂,Ki 为 4.5 nM。Dabigatran (BIBR 953) 也抑制凝血酶诱导的血小板聚集 (IC50=10 nM)。
Cas No.: 211914-51-1
名称: 3-(2-((4-carbamimidoylphenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoic acid
别名: BIBR953,BIBR 953,BIBR-953
SMILES: CN1C2=C(C=C(C=C2)C(=O)N(CCC(=O)O)C3=CC=CC=N3)N=C1CNC4=CC=C(C=C4)C(=N)N
分子式: C25H25N7O3
分子量: 471.51
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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) in 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. 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 . 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DCAPI1112 BIBR 953(Dabigatran) Dabigatran (BIBR 953),口服抗凝剂,是可逆的,竞争性的直接凝血酶 (thrombin) 抑制剂,Ki 为 4.5 nM。Dabigatran (BIBR 953) 也抑制凝血酶诱导的血小板聚集 (IC50=10 nM)。
DC1010 BIBR-1048 (Dabigatran etexilate) Dabigatran etexilate (BIBR 1048) 是具有口服活性的 Dabigatran 前药。Dabigatran etexilate 具有抗凝作用,可以预防心房颤动引起的静脉血栓栓塞和中风。