Vonoprazan Fumarate_product_DataBase

Bioactivity	Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease[1][2].
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 (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats[2]. Animal Model:
Name	Vonoprazan Fumarate
CAS	881681-01-2
Formula	C21H20FN3O6S
Molar Mass	461.46
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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),

PeptideDB

Vonoprazan Fumarate

CAS: 881681-01-2 F: C21H20FN3O6S W: 461.46