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Dabigatran etexilate mesylate Sale

(Synonyms: 甲磺酸达比加群酯; BIBR 1048MS; Dabigatran etexilate methanesulfonate) 目录号 : GC15390

A prodrug form of dabigatran

Dabigatran etexilate mesylate Chemical Structure

Cas No.:872728-81-9

规格 价格 库存 购买数量
5mg
¥439.00
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10mg
¥641.00
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50mg
¥1,170.00
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100mg
¥1,638.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Description: IC50 Value: 4.5nM (Ki); 10nM(Thrombin-induced platelet aggregation) [1] Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug,dabigatran etexilate. 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 [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

Chemical Properties

Cas No. 872728-81-9 SDF
别名 甲磺酸达比加群酯; BIBR 1048MS; Dabigatran etexilate methanesulfonate
化学名 ethyl 3-(2-(((4-(N-((hexyloxy)carbonyl)carbamimidoyl)phenyl)amino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate methanesulfonate
Canonical SMILES CCCCCCOC(NC(C1=CC=C(NCC2=NC3=C(C=CC(C(N(C4=CC=CC=N4)CCC(OCC)=O)=O)=C3)N2C)C=C1)=N)=O.CS(=O)(O)=O
分子式 C35H45N7O8S 分子量 723.84
溶解度 ≥ 36.192 mg/mL in DMSO, ≥ 45.8 mg/mL in EtOH with gentle warming 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.3815 mL 6.9076 mL 13.8152 mL
5 mM 0.2763 mL 1.3815 mL 2.763 mL
10 mM 0.1382 mL 0.6908 mL 1.3815 mL
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