Vonoprazan Fumarate (TAK-438)

Catalog No.S8016

Vonoprazan Fumarate (TAK-438) Chemical Structure

Molecular Weight(MW): 461.46

Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.

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In DMSO USD 500 In stock
USD 270 In stock
USD 370 In stock
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Biological Activity

Description Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.
Features Capable of inhibiting H+, K+-ATPase under acidic or neutral conditions.
Targets
H+/K+-ATPase [1]
19 nM
In vitro

TAK-438 is a pyrrole derivative with a chemical structure that is completely different from the P-CABs developed to date. TAK-438 inhibits gastric H+, K+-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 is almost the same as that under weakly acidic conditions (pH 6.5). TAK-438 does not inhibit Na+, K+-ATPase activity even at concentration 500 times higher than their IC50 values against gastric H+,K+-ATPase activity. TAK-438 inhibits gastric H+, K+-ATPase in a K+-competitive manner with Ki of 3 nM. [2]

In vivo TAK-438 inhibits basal gastric acid secretion in a dose-dependent manner, and the ID50 value is 1.26 mg/kg . Intravenous administration of TAK-438 dose-dependently increases the pH of the gastric perfusate, and the increase in pH is sustained for 5 h after administration. At the 1 mg/kg dose, the pH plateaues 90 min after administration, and the highest pH value reached is 5.9. [2] In addition, TAK-438 shows a potent and longer-lasting inhibitory effect on the histamine-stimulated gastric acid secretion in rats and dogs. TAK-438 shows significant antisecretory activity through high accumulation and slow clearance from the gastric tissue. TAK-438 is unaffected by the gastric secretory state, unlike PPIs. [3]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: Male Sprague-Dawley rats
  • Formulation: 0.5% methylcellulose solution
  • Dosages: 1, 2, and 4 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL (134.35 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
0.5% methylcellulose
17 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.46
Formula

 

C17H16FN3O2S.C4H4O4
CAS No. 1260141-27-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03050307 Not yet recruiting Gastric Ulcer|Peptic Ulcer|Gastrointestinal Diseases|Digestive System Diseases|Lansoprazole|Anti-Ulcer Agents|Gastrointestinal Agents|Proton Pump Inhibitors|Enzyme Inhibitors|Molecular Mechanisms of Pharmacological Action Takeda April 2017 Phase 3
NCT03050359 Not yet recruiting Duodenal Ulcer Takeda April 2017 Phase 3
NCT02954848 Recruiting Non-erosive Gastroesophageal Reflux Disease Takeda December 2016 Phase 3
NCT02892409 Recruiting Helicobacter Pylori Takeda September 2016 Phase 1
NCT01630746 Completed Erosive Esophagitis Takeda July 2012 Phase 3
NCT01568398 Completed Gastric Ulcer|Duodenal Ulcer Takeda May 2012 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID