Dabigatran (BIBR-1048) etexilate

CAS: 211915-06-9 货号: D408215 分子式: C34H41N7O5 分子量: 627.73 PubChem CID: 6445226
有货
级别和纯度: Moligand™ ? Moligand™ —— 阿拉丁的配体和生物活性小分子系列。适用于需要明确小分子工具的受体、通路和结合研究。 10mM in DMSO
别名
达比加群酯(BIBR-1048)
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
D408215-1ml
现货 Stock Image
¥871.90
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为什么选择此级别

Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 4 篇同行评审文献引用。

概述

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。

Information

Dabigatran (BIBR-1048) etexilate Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombi
In vitro

Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent 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 μM, respectively. [1]

In vivo

Dabigatran prolongs 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). Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥97%

规格

别名
达比加群酯(BIBR-1048)
英文别名
(E)-ethyl 3-(2-((4-(N'-(hexyloxycarbonyl)carbamimidoyl)phenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Dabigatran (BIBR-1048) etexilate
生化机理
达比加群酯(Dabigatran Etexilate)(BIBR-1048)是达比加群的原药,它是一种强效的非肽小分子,通过与凝血酶分子的活性位点结合,特异性地、可逆性地抑制游离的和与血块结合的凝血酶。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCCCCCOC(=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
PubChem CID
分子量
627.73

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

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✅ 分析证书 (COA)

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🔬 规格说明书

该级别的完整质量属性和验收标准。

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高级数据

化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (128.05 mM); Water: Insoluble; Ethanol: Insoluble;
熔点
131 °C
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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此产品的引用文献
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