达比加群.|211914-51-1|(达比加群; BIBR 953; BIBR 953ZW)-陌孚医药/Medlife

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达比加群. (Synonyms: 达比加群; BIBR 953; BIBR 953ZW)

目录号: PC15670 纯度: ≥98%

CAS No. :211914-51-1

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中文名称

达比加群.

中文别名

达比加群;N-[[2-[[[4-(氨基亚氨基甲基)苯基]氨基]甲基]-1-甲基-1H-苯并[D]咪唑-5-基]羰基]-N-吡啶-2-基-BETA-丙氨酸;4-(4-(4-硝基苯基)-1-哌嗪基)苯酚;Dabigatran (BIBR 953) 抑制剂;N-[[2-[[[4-(氨咪甲基)苯基]氨基]甲基]-1-甲基-1H-苯并咪唑-5-基]羰基]-N-2-吡啶基-β-丙氨酸;达比加群-D4;达比加群标准品;达比加群杂质;达比加群酯;达比加群酯杂质A;尾-Alanine,N-[[2-[[[4-(aminoiminomethyl)phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carb...

英文名称

3-[[2-[[(4-carbamimidoylphenyl)amino]methyl]-1-methyl-benzoimidazole-5-carbonyl]-pyridin-2-yl-amino]propanoic acid

英文别名

3-[[2-[[(4-carbamimidoylphenyl)amino]methyl]-1-methyl-benzoimidazole-5-carbonyl]-pyridin-2-yl-amino]propanoic acid;BIB-953;BIBR 953;Dabigatran;BIBR 953ZW;BIBR 953(Dabigatran);Dabigatran (BIBR 953);Dabigatran Etexilate Mesilate;BIBR 953 (Dabigatran, Pradaxa);3-[[2-[[(4-carbaMiMidoylphenyl)aMino]Methyl]-1-Met;N- (2-{ (4-carbaMiMidoylphenyl)aMino Methyl}-1-Met;3-[[2-[(4-carbamimidoylanilino)methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoic acid;β-Alanine, N-[[2-[[[4-(aminoiminomethyl)phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-;N-[[2-[[[4-(aminoiminomethyl)phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-Alanine;BIBR 953,Dabigatran,BIBR953;BIBR-953;UNII-I0VM4M70GC;3-(2-(((4-carbamimidoylphenyl)amino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoic acid

Cas No.

211914-51-1

分子式

C₂₅H₂₅N₇O₃

分子量

471.51

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (K_i=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC₅₀=10 nM).

性状

Solid

IC50 & Target[1][2]

Ki: 4.5 nM (thrombin)

体外研究(In Vitro)

Dabigatran (BIBR 953) shows concentration-dependent anticoagulant effects in various species 体外研究, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human platelet-poor plasma at concentrations of 0.23, 0.83 and 0.18 μM, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits clot formation with an ED₅₀ of 0.033 mg/kg in Wessler model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male rats (Wessler model)
Dosage:	0.01, 0.03, 0.05 and 0.1 mg/kg
Administration:	Intravenous injection
Result:	Inhibited clot formation with an ED₅₀ of 0.033 mg/kg.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Wienen W, Stassen JM, Priepke H, In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62. [Information]

[2]. Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66. [Information]

[3]. Wienen W, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007 Aug;98(2):333-8. [Information]

溶解度数据

体外研究:

0.1 M HCL : 12.5 mg/mL (26.51 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1208 mL	10.6042 mL	21.2085 mL
5 mM	0.4242 mL	2.1208 mL	4.2417 mL
10 mM	0.2121 mL	1.0604 mL	2.1208 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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