Vonoprazan hydrochloride  (Synonyms: TAK-438 hydrochloride)

Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H⁺,K⁺-ATPase activity in porcine gastric microsomes with an IC₅₀ of 19 nM at pH 6.5. Vonoprazan hydrochloride is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride can be used for eradication of Helicobacter pylori^[1][2][3].

IC₅₀: 19 nM (porcine gastric H⁺,K⁺-ATPase, at pH 6.5)^[2]

Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H⁺, K⁺-ATPase activity in a concentration-dependent manner^[2].
Vonoprazan does not inhibit Na⁺,K⁺-ATPase activity, even at concentrations 500 times higher than their IC₅₀ values against gastric H⁺,K⁺-ATPase activity^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

381.85

C₁₇H₁₇ClFN₃O₂S

1957202-44-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456.  [Content Brief]

  [2]. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1),  [Content Brief]

  [3]. Sugimoto M, et al. Role of Vonoprazan in Helicobacter pylori Eradication Therapy in Japan. Front Pharmacol. 2019 Jan 15;9:1560.  [Content Brief]