Dabigatran

製品コードS2196 バッチS219602

印刷

化学情報

Chemical Structure Synonyms BIBR 953 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H25N7O3
分子量 471.51 CAS No. 211914-51-1
Solubility (25°C)* 体外 DMSO Insoluble
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Dabigatranは、強力な非ペプチド・トロンビン阻害剤で、IC50 が9.3 nMです。
in vitro BIBR 953 is a very potent anticoagulant. This compound shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. It inhibits thrombin, plasmin, factor Xa, trypsin, tPA and activated protein C with Ki of 4.5 nM, 1.7 μM, 3.8 μM, 50 nM, 45 μM and 20 μM, respectively. [1] This chemical specifically and reversibly inhibits thrombin. [2]
in vivo BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. [1] The bioavailability of this compound after p.o. administration of dabigatran etexilate is 7.2%. It is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of this chemical is approximately 8 hours. Its acylglucuronides accounts for 0.4% and 4% of the dose in urine after p.o. and i.v. dosing, respectively. [3]
特徴 Dabigatran is a reversible, competitive, direct thrombin inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ Measurement of thrombin inhibition
The thrombin inhibitory effects (IC50) of Dabigatran is determined with a commercially available chromogenic assay. Human thrombin (0.042 U/mL) is preincubated for 10 minutes at 37 °C with 10 different dilutions (concentration range of 0.003 μM -100 μM) of this compound dissolved in DMSO or with DMSO as control. Upon addition of the preincubation mixture to the chromogenic substrate, tosyl-glycyl-prolyl-arginine-4-nitranilide acetate, nitraniline is cleaved by thrombin and the increase in absorbance at 405 nm, related to the free nitraniline, is measured in a spectrophotometer. By plotting the absorbance at 405 nm vs the concentration of this chemical, the concentration that induces a 50% thrombin inhibition (IC50) is calculated. All measurements are performed in duplicate, and the mean values of both determinations are represented.
動物実験 動物モデル Rats
投薬量
投与方法 Administered via i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/11960487/
  • https://pubmed.ncbi.nlm.nih.gov/17506785/
  • https://pubmed.ncbi.nlm.nih.gov/18006647/

カスタマーフィードバック

Data from [Thromb Res, 2014, 133 Suppl 1, S6-8]

, , J Thromb Thrombolysis, 2017, 44(2):216-222

Data from [Data independently produced by , , Sci Rep, 2016, 6:29387]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HemoDens: A global hemostasis analyzer for kinetic characterization of clot formation, retraction, and lysis [ Thromb Res, 2025, 255:109480] PubMed: 40987075
Real-Time Imaging of Platelet-Initiated Plasma Clot Formation and Lysis Unveils Distinct Impacts of Anticoagulants [ Thromb Haemost, 2025, 10.1055/a-2497-4213] PubMed: 39788528
Dabigatran Attenuates the Binding of Thrombin to Platelets-A Novel Mechanism of Action [ Thromb Haemost, 2024, 10.1055/a-2483-0107] PubMed: 39586831
Detection of direct oral anticoagulants with the diluted Russel's viper venom time [ Int J Lab Hematol, 2024, 10.1111/ijlh.14300] PubMed: 38721750
DPP4 inhibition impairs senohemostasis to improve plaque stability in atherosclerotic mice [ J Clin Invest, 2023, 133(12)e165933] PubMed: 37097759
OKL-1111, A modified cyclodextrin as a potential universal reversal agent for anticoagulants [ Thromb Res, 2023, 227:17-24] PubMed: 37207560
Thrombin induces ACSL4-dependent ferroptosis during cerebral ischemia/reperfusion [ Signal Transduct Target Ther, 2022, 7(1):59] PubMed: 35197442
Scanning laser-induced endothelial injury: a standardized and reproducible thrombosis model for intravital microscopy [ Sci Rep, 2022, 12(1):3955] PubMed: 35273275
Aortic intimal resident macrophages are essential for maintenance of the non-thrombogenic intravascular state [ Nat Cardiovasc Res, 2022, 1(1):67-84] PubMed: 35599984
Induced forms of α2-macroglobulin neutralize heparin and direct oral anticoagulant effects [ Int J Biol Macromol, 2021, 184:209-217] PubMed: 34126147

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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