Home Transmembrane Transporters Potassium Channel inhibitor Vonoprazan Fumarate (TAK-438) For research use only.

Vonoprazan Fumarate (TAK-438)

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

Vonoprazan Fumarate (TAK-438) Chemical Structure

CAS No. 1260141-27-2

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Vonoprazan Fumarate (TAK-438) Related Products

Signaling Pathway

Potassium Channel Signaling Pathways

Potassium Channel Signaling Pathway

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
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
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]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 1, 2, and 4 mg/kg
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03808493 Completed
Japanese Healthy Adult Male
Takeda
 January 30 2019 Phase 1
NCT03456960 Completed
Healthy Volunteers
Takeda
 March 8 2018 Phase 1
NCT03085836 Completed
Healthy Participants
Takeda
 April 19 2017 Phase 1
NCT02774902 Completed
Healthy Volunteers
Takeda
 August 2010 Phase 1
NCT02141711 Completed
Erosive Esophagitis(EE)|Gastroesophageal Reflux Disease (GERD)
Takeda
 October 2008 Phase 1
NCT02123953 Completed
Dose Finding Study
Takeda
 October 2008 Phase 1

Chemical Information & Solubility

Molecular Weight 461.46 Formula

 

C17H16FN3O2S.C4H4O4
CAS No. 1260141-27-2 SDF Download Vonoprazan Fumarate (TAK-438) SDF
Smiles CNCC1=CN(C(=C1)C2=CC=CC=C2F)S(=O)(=O)C3=CN=CC=C3.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (134.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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