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Pumaprazole

MCE China：Pumaprazole

Brand：MedChemExpress (MCE)

Cat. No.HY-19223

CAS：158364-59-1

Synonyms：BY-841

Purity：99.75%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Pumaprazole is a reversible proton pump antagonist.

In Vivo：Pumaprazole is a reversible proton pump antagonist. Basal acid secretion in the Ghosh-Schild rat is inhibited by Pumaprazole with a higher efficacy compare to ranitidine. Pumaprazole displays identical ID50 values on day 1 (11 μmol/kg, 95% confidence limits of 5 and 23) and on day 7 (10 μmol/kg, 95% confidence limits of 4 and 23) of a repeated dose study in this model. The lower dose of Pumaprazole (27 μmol/kg) rapidly elevates luminal pH up to almost neutrality, the higher dose (54 μmol/kg) further prolongs this pH-elevating effect[1].

Animal Administration：The pylorus of female Sprague-Dawley rats (160 to 220 g body weight) is ligated under ether anesthesia, the abdomen is closed and 100 mg/kg of acetylsalicylic acid (ASA) in 10 mL/kg are given orally. Following ASA administration, Pumaprazole (solution) or vehicle (i.v. saline or tap water in case of oral administration) is given i.v. in 1 mL/kg or i.d. in 2.5 mL/kg. Oral drug administration (in 10 mL/kg) is 1 h before pylorus ligation. Four hours after pylorus ligation, the stomach is excised, carefully keeping the esophagus closed, opened along the greater curvature and the luminal contents are removed, centrifuged, the volume is measured and the acidity determined by titration with 0.1 N NaOH to pH 7[1].

IC50 & Target：proton pump[1] In Vivo Pumaprazole is a reversible proton pump antagonist. Basal acid secretion in the Ghosh-Schild rat is inhibited by Pumaprazole with a higher efficacy compare to ranitidine. Pumaprazole displays identical ID50 values on day 1 (11 μmol/kg, 95% confidence limits of 5 and 23) and on day 7 (10 μmol/kg, 95% confidence limits of 4 and 23) of a repeated dose study in this model. The lower dose of Pumaprazole (27 μmol/kg) rapidly elevates luminal pH up to almost neutrality, the higher dose (54 μmol/kg) further prolongs this pH-elevating effect[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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References：

[1]. Kromer W, et al. Animal pharmacology of reversible antagonism of the gastric acid pump, compared to standard antisecretory principles. Pharmacology. 2000 May;60(4):179-87.  [Content Brief]