Dabigatran

製品コードS2196 バッチS219605

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 5%TFA 6.09 mg/mL (12.91 mM)
DMSO Insoluble
Water 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. This chemical specifically and reversibly inhibits thrombin.
in vivo BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. 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.
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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