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Vonoprazan Fumarate

Catalog No. T21254   CAS 881681-01-2
Synonyms: TAK-438, TAK 438, Vonoprazan Fumurate, TAK438

Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.

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Vonoprazan Fumarate Chemical Structure
Vonoprazan Fumarate, CAS 881681-01-2
Pack Size Availability Price/USD Quantity
100 mg In stock $ 41.00
200 mg In stock $ 65.00
500 mg In stock $ 141.00
1 mL * 10 mM (in DMSO) In stock $ 45.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.
Targets&IC50 H+,K+-ATPase:19 nM
In vitro The inhibitory activity of Vonoprazan Fumurate was unaffected by ambient pH. The inhibition by Vonoprazan Fumurate was reversible and achieved in a K(+)-competitive manner, quite different from that by lansoprazole. Vonoprazan Fumurate exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner[4].
In vivo Vonoprazan Fumurate, at a dose of 4 mg/kg (as the free base) orally, completely inhibited basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats, and its effect on both was stronger than that of lansoprazole. Vonoprazan Fumurate increased the pH of gastric perfusate to a higher value than did lansoprazole or SCH28080, and the effect of Vonoprazan Fumurate was sustained longer than that of lansoprazole or SCH28080[4].
Synonyms TAK-438, TAK 438, Vonoprazan Fumurate, TAK438
Molecular Weight 461.46
Formula C21H20FN3O6S
CAS No. 881681-01-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.61 mg/mL (10 mM), Sonification is recommended

TargetMolReferences and Literature

1. Masaoka T, et al. Pathophysiology of Potassium-competitive Acid Blocker-refractory Gastroesophageal Reflux and the Potential of Potassium-competitive Acid Blocker Test. J Neurogastroenterol Motil. 2018 Oct 1;24(4):577-583. 2. 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. 3. Sugano K. Vonoprazan fumarate, a novel potassium-competitive acid blocker, in the management of gastroesophageal reflux disease: safety and clinical evidence to date. Therap Adv Gastroenterol. 2018 Jan 9;11:1756283X17745776. 4. 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), 231-238.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Orally Active Compound Library FDA-Approved Drug Library Exosome Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library Approved Drug Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Keywords

Vonoprazan Fumarate 881681-01-2 Membrane transporter/Ion channel Proton pump peptic potassium TAK-438 secretion reflux competitive TAK 438 proton inhibitor antisecretory disease gastroesophageal Vonoprazan Fumurate inhibit Vonoprazan ulcer GERD blocker acid gastric TAK438 pump P-CAB Proton Pump

 

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