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Vonoprazan fumarate

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Catalog No. T2404Cas No. 1260141-27-2
Alias TAK-438

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

Vonoprazan fumarate

Vonoprazan fumarate

🥰Excellent
Purity: 100%
Catalog No. T2404Alias TAK-438Cas No. 1260141-27-2
Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase.
Pack SizePriceAvailabilityQuantity
500 mg$40In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Product Introduction

Bioactivity
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.
AliasTAK-438
Chemical Properties
Molecular Weight461.46
FormulaC17H16FN3O2S·C4H4O4
Cas No.1260141-27-2
SmilesCNCc1cn(c(c1)c1ccccc1F)S(=O)(=O)c1cnccc1.C(=C\C(=O)O)/C(=O)O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16.67 mg/mL (36.12 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1670 mL10.8352 mL21.6704 mL108.3518 mL
5 mM0.4334 mL2.1670 mL4.3341 mL21.6704 mL
10 mM0.2167 mL1.0835 mL2.1670 mL10.8352 mL
20 mM0.1084 mL0.5418 mL1.0835 mL5.4176 mL

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