Vonoprazan Fumarate (TAK-438)

Catalog No.S8016

For research use only.

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.

Vonoprazan Fumarate (TAK-438) Chemical Structure

CAS No. 1260141-27-2

Purity & Quality Control

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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 (from reference)

Animal Research:[3]
  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 1, 2, and 4 mg/kg
  • Administration: Orally

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.

17 mg/mL

Chemical Information

Molecular Weight 461.46
Formula

 

C17H16FN3O2S.C4H4O4
CAS No. 1260141-27-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNCC1=CN(C(=C1)C2=CC=CC=C2F)S(=O)(=O)C3=CN=CC=C3.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03808493 Completed Drug: TAK-438 OD|Drug: TAK-438 Japanese Healthy Adult Male Takeda January 30 2019 Phase 1
NCT03456960 Completed Drug: TAK-438ASA|Drug: TAK-438|Drug: Aspirin Healthy Volunteers Takeda March 8 2018 Phase 1
NCT03085836 Completed Drug: TAK-438 Healthy Participants Takeda April 19 2017 Phase 1
NCT02774902 Completed Drug: TAK-438|Drug: Clarithromycin Healthy Volunteers Takeda August 2010 Phase 1
NCT02141711 Completed Drug: TAK-438|Drug: TAK-438 Placebo Erosive Esophagitis(EE)|Gastroesophageal Reflux Disease (GERD) Takeda October 2008 Phase 1
NCT02123953 Completed Drug: TAK-438|Drug: TAK-438 Placebo Dose Finding Study Takeda October 2008 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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