1. Membrane Transporter/Ion Channel
  2. Proton Pump
  3. Vonoprazan Fumarate

Vonoprazan Fumarate (Synonyms: TAK-438)

Cat. No.: HY-15295 Purity: 99.94%
Handling Instructions

Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.

For research use only. We do not sell to patients.

Vonoprazan Fumarate Chemical Structure

Vonoprazan Fumarate Chemical Structure

CAS No. : 881681-01-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
250 mg USD 100 In-stock
Estimated Time of Arrival: December 31
500 mg USD 170 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease[1][2].

IC50 & Target

IC50: 19 nM (porcine gastric H+,K+-ATPase, at pH 6.5)[2]

In Vitro

Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner[2].
Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male 7- or 8-week-old Sprague-Dawley rat[2]
Dosage: 0.5, 1, 2, and 4 mg/kg
Administration: Oral administration
Result: Inhibited basal gastric acid secretion in a dose-dependent manner.
Molecular Weight

461.46

Formula

C₂₁H₂₀FN₃O₆S

CAS No.

881681-01-2

SMILES

O=C(O)/C=C/C(O)=O.O=S(N1C=C(CNC)C=C1C2=CC=CC=C2F)(C3=CC=CN=C3)=O.[(E)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (108.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1670 mL 10.8352 mL 21.6704 mL
5 mM 0.4334 mL 2.1670 mL 4.3341 mL
10 mM 0.2167 mL 1.0835 mL 2.1670 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.94%

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Keywords:

VonoprazanTAK-438TAK438TAK 438Proton PumpantisecretorygastricacidsecretionprotonpumpinhibitorblockerpotassiumcompetitiveP-CABgastroesophagealrefluxdiseaseGERDpepticulcerInhibitorinhibit

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Vonoprazan Fumarate
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