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Vonoprazan fumarate

Catalog No. T2404 CAS 1260141-27-2

Synonyms: TAK-438

Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase.

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Vonoprazan fumarate, CAS 1260141-27-2

Pack Size	Availability	Price/USD
100 mg	In stock	$ 39.00
500 mg	In stock	$ 139.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 100%

Purity: 99.16%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase.
Targets&IC50	H+, K+-ATPase:19 nM
In vitro	TAK-438 has demonstrated effective and sustained inhibition of gastric acid secretion stimulated by histamine in both rats and dogs. This compound exhibits notable antisecretory activity through its high accumulation in gastric tissue and low clearance rate. Unlike PPIs (Proton Pump Inhibitors), TAK-438's efficacy is not influenced by the state of gastric secretion. It inhibits basal gastric acid secretion in a dose-dependent manner, with an ID50 value of 1.26 mg/kg. Intravenous administration of TAK-438 increases the pH of gastric perfusate in a dose-dependent way, maintaining the rise in pH for up to five hours. When treated with 1 mg/kg of TAK-438, the pH value reached a stable state after 90 minutes, with a maximum pH of 5.9.
In vivo	TAK-438 inhibits the activity of gastric H+,K+-ATPase in a concentration-dependent manner. Its inhibitory effect remains almost unchanged under neutral (pH 7.5) and slightly acidic conditions (pH 6.5). Even at concentrations 500 times higher than its IC50 for gastric H+,K+-ATPase activity, TAK-438 does not inhibit Na+,K+-ATPase activity. TAK-438 inhibits gastric H+,K+-ATPase competitively with potassium (K+), with an inhibition constant (Ki) of 3 nM.

Synonyms	TAK-438
Molecular Weight	461.46
Formula	C17H16FN3O2S·C4H4O4
CAS No.	1260141-27-2

Storage

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

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 58 mg/mL (125.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Arikawa Y, et al. J Med Chem, 2012, 55(9), 4446-4456. 2. Hori Y, et al. J Pharmacol Exp Ther, 2010, 335(1), 231-238. 3. Hori Y, et al. J Pharmacol Exp Ther, 2011, 337(3), 797-804.

Related compound libraries

This product is contained In the following compound libraries：

Ion Channel Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Infection Compound Library Immunology/Inflammation Compound Library NO PAINS Compound Library Fluorochemical Library

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Keywords

Vonoprazan fumarate 1260141-27-2 Membrane transporter/Ion channel ATPase TAK 438 TAK438 TAK-438 Vonoprazan Fumarate inhibitor inhibit

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