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Synonyms | BIBR 953 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H25N7O3 |
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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. |
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。 |
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in vitro | BIBR 953 is a very potent anticoagulant. BIBR 953 shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. BIBR 953 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] BIBR 953 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 dabigatran after p.o. administration of dabigatran etexilate is 7.2%. Dabigatran is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of dabigatran is approximately 8 hours. Dabigatran 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. |
キナーゼアッセイ | Measurement of thrombin inhibition | |
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The thrombin inhibitory effects (IC50) of BIBR 953 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 BIBR 953 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 BIBR 953, 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. |
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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]
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 |
Unveiling the complex effects of direct oral anticoagulants on dilute Russell's viper venom time assays [ J Thromb Haemost, 2020, 18(8):1866-1873] | PubMed: 32294291 |
Unveiling the complex effects of direct oral anticoagulants on dilute Russell's viper venom time assays [ Journal of Thrombosis and Haemostasis, 2020, 1866-1873] | PubMed: None |
An engineered factor Va prevents bleeding induced by direct-acting oral anticoagulants by different mechanisms [ Blood Adv, 2020, 4(15):3716-3727] | PubMed: 32777068 |
Whole Blood Point-of-Care Testing for Incomplete Reversal With Idarucizumab in Supratherapeutic Dabigatran. [ Anesth Analg, 2020, 130(2):535-541] | PubMed: 31490820 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。