Dabigatran

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Dabigatran

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

211914-51-1

达比加群
BIBR 953
BIBR 953ZW

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，K_i为 4.5 nM。Dabigatran (BIBR 953) 也抑制凝血酶诱导的血小板聚集 (IC₅₀=10 nM)。

生物活性

Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive directthrombininhibitor (K_i=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC₅₀=10 nM)^[1]^[2].

IC₅₀& Target

Ki: 4.5 nM (thrombin)^[1]

体外研究
(In Vitro)

Dabigatran (BIBR 953) shows 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 platelet-poor plasma at concentrations of 0.23, 0.83 and 0.18 μM, respectively^[1].

体内研究
(In Vivo)

Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits clot formation with an ED₅₀of 0.033 mg/kg in Wessler model^[3].

Animal Model:	Male rats (Wessler model)^[3]
Dosage:	0.01, 0.03, 0.05 and 0.1 mg/kg
Administration:	Intravenous injection
Result:	Inhibited clot formation with an ED₅₀of 0.033 mg/kg.

Clinical Trial

分子量

471.51

性状

Solid

Formula

C₂₅H₂₅N₇O₃

CAS 号

211914-51-1

中文名称

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运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。