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: 1260141-27-2

Purity & Quality Control

Batch: Purity: 99.03%
99.03

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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
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 lnformation & 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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