Vonoprazan hydrochloride

CAS: 1957202-44-6 F: C17H17ClFN3O2S W: 381.85

Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocke

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Bioactivity	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].
Target	IC50: 19 nM (porcine gastric H+,K+-ATPase, at pH 6.5)
Invitro	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].
In Vivo	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]. Animal Model:
Name	Vonoprazan hydrochloride
CAS	1957202-44-6
Formula	C17H17ClFN3O2S
Molar Mass	381.85
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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), [3]. Sugimoto M, et al. Role of Vonoprazan in Helicobacter pylori Eradication Therapy in Japan. Front Pharmacol. 2019 Jan 15;9:1560.