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BIBR 953 (Dabigatran, Pradaxa) Sale

(Synonyms: 达比加群; BIBR 953; BIBR 953ZW) 目录号 : GC16293

A thrombin inhibitor

BIBR 953 (Dabigatran, Pradaxa) Chemical Structure

Cas No.:211914-51-1

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5mg
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10mg
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Thrombin inhibition assay [1]:

Chromogenic assay

Human thrombin (0.042 U/mL) was pre-incubated for 10 mins at 37 °C with 10 different dilutions (concentration range of 0.003 ~ 100 μM) of BIBR 953 dissolved in DMSO or with DMSO as control. Upon addition of the pre-incubation mixture to the chromogenic substrate, tosyl-glycyl-prolyl-arginine-4-nitranilide acetate, nitraniline was cleaved by thrombin and the increase in absorbance at 405 nm, related to the free nitraniline, was measured in a spectrophotometer. By plotting the absorbance at 405 nm vs the concentration of the test compound, IC50 was calculated.

In intro experiment [2]:

Samples

Adult and neonatal platelet-poor plasma

Preparation method

The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0, 40, 110, 180, 250 or 320 ng/mL

Applications

Without the presence of BIBR 953, neonatal and adult samples showed similar results on the time to clot initiation. In neonatal samples, BIBR 953 significantly delay clotting in a dose-dependent manner, with the difference increasing from 3 times for 40 ng/mL BIBR 953 to 9 times for 320 ng/mL BIBR 953.

Animal experiment [1]:

Animal models

Rats

Dosage form

i.v.

Applications

Compared with all of the inhibitors tested, BIBR 953 exhibited the strongest activity and the longest duration of action. Besides, it was well-tolerated in rats up to the highest dose of 10 mg/kg. However, BIBR 953 was not orally active because it was a very polar, a permanently charged molecule with a logP of -2.4 (n-octanol/buffer, pH 7.4).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Hauel NH, Nar H, Priepke H, Ries U, Stassen JM, Wienen W. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.

[2]. Nossair FF, Chan HHW, Gantioqui J, Atkinson HM, Berry LR, Chan AKC. In-vitro assessment of the effect of dabigatran on thrombosis of adult and neonatal plasma: comparisons using thromboelastography and microscopic visualization of fibrin clot structure. Blood Coagul Fibrinolysis. 2017 May 12.

产品描述

BIBR 953 is a potent, reversible, and direct inhibitor of thrombin with IC50 value of 9.3nM [1].

BIBR 953 shows a favorable selectivity profile and strong activity in vitro with a Ki value of 4.5nM. It also exhibits the best activity profile in vivo following administration to rats. BIBR 953 is designed to be converted into an orally active prodrug BIBR 1048 due to its highly polar, zwitterionic nature and poor oral absorption. BIBR 953 inhibits thrombin in a competitive fashion. This inhibition is rapid and reversible. BIBR 953 inhibits both clot-bound and free thrombin. BIBR 953 is demonstrated to have an anticoagulant efficacy both in vitro and ex vivo. Since thrombin can affect cell behavior and response in various tissue types via PAR signaling, BIBR 953 is found to be beneficial in many diseases including inflammation, infection, fibrosis and cancer. Clinical trials show that BIBR 953 is a highly effective anticoagulant with a good safety profile [1, 2].

References:
[1] Hauel NH, Nar H, Priepke H, Ries U, Stassen JM, Wienen W. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.
[2] van Ryn J, Goss A, Hauel N, Wienen W, Priepke H, Nar H, Clemens A. The discovery of dabigatran etexilate. Front Pharmacol. 2013 Feb 12;4:12.

Chemical Properties

Cas No. 211914-51-1 SDF
别名 达比加群; BIBR 953; BIBR 953ZW
化学名 3-[[2-[(4-carbamimidoylanilino)methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoic acid
Canonical 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 471.5
溶解度 12.5 mg/mL in 0.1 M HCL (Need ultrasonic); < 0.1 mg/mL in Water; < 1 mg/mL in DMSO. 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 2.1209 mL 10.6045 mL 21.2089 mL
5 mM 0.4242 mL 2.1209 mL 4.2418 mL
10 mM 0.2121 mL 1.0604 mL 2.1209 mL
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