Picoprazole
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
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- CAS 番号: 78090-11-6
- 分子式: C17H17N3O3S
- 分子量:343.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 3.1±0.4 μM (H+/K+-ATPase)[1]
Picoprazole inhibits the H+/K+-ATPase activity in a concentration-dependent manner. The IC50 value is 3.1±0.4 μM[1]. Picoprazole is a specific inhibitor of H+/K+-ATPase and binds to 100-kDa polypeptides of the enzyme, dose dependently inhibited opening of the Cl- conductance by Cu2+-o-phenanthroline, indicating that the Cl- conductance is part of the function of the H+/K+-ATPase[2]. The inhibitory effect of the three benzimidazole derivatives Timoprazole, Picoprazole, and Omeprazole on histamine and dbcAMP stimulated 14C-aminopyrine accumulation (H+ secretion) has been studied in isolated and enriched guinea-pig parietal cells. All compounds tested inhibit H+ secretion in a concentration dependent manner with IC50 values of 8.5±1.9 μM for Timoprazole, 3.9±0.7 μM for Picoprazole, and 0.13±0.03 μM for Omeprazole[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 78090-11-6
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分子量 343.40
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分子式 C17H17N3O3S
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SMILES
O=C(C1=C(C)C=C2N=C(S(CC3=NC=CC=C3C)=O)NC2=C1)OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Beil W, et al. Inhibition of partially purified H+/K+-ATPase from guinea-pig isolated and enriched parietal cells by substituted benzimidazoles. Br J Pharmacol. 1984 Jul;82(3):651-7. [Content Brief]
[2]. Takeguchi N, et al. Disulfide cross-linking of H,K-ATPase opens Cl- conductance, triggering proton uptake in gastric vesicles. Studies with specific inhibitors. J Biol Chem. 1986 Feb 25;261(6):2560-6. [Content Brief]
[3]. Sewing KF, et al. Effect of substituted benzimidazoles on acid secretion in isolated and enriched guinea pig parietal cells. Gut. 1983 Jun;24(6):557-60. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Picoprazole 関連分類
HY-15384 関連分類
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