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Vonoprazan Fumarate (TAK-438) Potassium Channel inhibitor

Name: Vonoprazan Fumarate (TAK-438)
Brand: Selleck Chemicals
SKU: S8016
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8016

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), and controls gastric acid secretion. This compound is in Phase 3.

Chemical Structure

Molecular Weight: 461.46

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.65%

99.65

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Chemical Information, Storage & Stability

Molecular Weight	461.46	Formula	C₁₇H₁₆FN₃O₂S.C₄H₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1260141-27-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CNCC1=CN(C(=C1)C2=CC=CC=C2F)S(=O)(=O)C3=CN=CC=C3.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% methylcellulose Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (21.67mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Capable of inhibiting H+, K+-ATPase under acidic or neutral conditions.
Targets/IC₅₀/Ki	H+/K+-ATPase ^[1] 19 nM
In vitro	Vonoprazan Fumarate (TAK-438) is a pyrrole derivative with a chemical structure that is completely different from the P-CABs developed to date. It inhibits gastric H⁺, K⁺-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of this compound is almost the same as that under weakly acidic conditions (pH 6.5). It does not inhibit Na⁺, K⁺-ATPase activity even at concentration 500 times higher than their IC50 values against gastric H+,K+-ATPase activity. This compound inhibits gastric H⁺, K⁺-ATPase in a K⁺-competitive manner with K_i of 3 nM. ^[2]
In vivo	Vonoprazan Fumarate (TAK-438) inhibits basal gastric acid secretion in a dose-dependent manner, and the ID50 value is 1.26 mg/kg. Intravenous administration of this compound 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, it shows a potent and longer-lasting inhibitory effect on the histamine-stimulated gastric acid secretion in rats and dogs. It shows significant antisecretory activity through high accumulation and slow clearance from the gastric tissue. This compound is unaffected by the gastric secretory state, unlike PPIs. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/22512618/ [2] https://pubmed.ncbi.nlm.nih.gov/20624992/ [3] https://pubmed.ncbi.nlm.nih.gov/21411494/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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