Vonoprazan (Synonyms: TAK-438 free base)

Name: Vonoprazan
Brand: MedChemExpress
SKU: HY-100007
Rating: 5.0 (5 reviews)

Cat. No.: HY-100007 Purity: 99.52%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

Vonoprazan Chemical Structure

CAS No. : 881681-00-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
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100 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
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Based on 5 publication(s) in Google Scholar

Other Forms of Vonoprazan:

5 Publications Citing Use of MCE Vonoprazan

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Description

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].

MedChemExpress (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 (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats^[2].

MedChemExpress (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 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg
Administration:	Oral administration
Result:	Inhibited basal gastric acid secretion in a dose-dependent manner.

Clinical Trial

Molecular Weight

345.40

Formula

C₁₇H₁₆FN₃O₂S

CAS No.

881681-00-1

Appearance

Solid

Color

White to off-white

SMILES

O=S(N1C=C(CNC)C=C1C2=CC=CC=C2F)(C3=CC=CN=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (289.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8952 mL	14.4760 mL	28.9520 mL
5 mM	0.5790 mL	2.8952 mL	5.7904 mL
10 mM	0.2895 mL	1.4476 mL	2.8952 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.52%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (257 KB) HNMR (257 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456. [Content Brief]

[2]. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1), 231-238. [Content Brief]

[3]. Sugimoto M, et al. Role of Vonoprazan in Helicobacter pylori Eradication Therapy in Japan. Front Pharmacol. 2019 Jan 15;9:1560. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8952 mL	14.4760 mL	28.9520 mL	72.3801 mL
	5 mM	0.5790 mL	2.8952 mL	5.7904 mL	14.4760 mL
	10 mM	0.2895 mL	1.4476 mL	2.8952 mL	7.2380 mL
	15 mM	0.1930 mL	0.9651 mL	1.9301 mL	4.8253 mL
	20 mM	0.1448 mL	0.7238 mL	1.4476 mL	3.6190 mL
	25 mM	0.1158 mL	0.5790 mL	1.1581 mL	2.8952 mL
	30 mM	0.0965 mL	0.4825 mL	0.9651 mL	2.4127 mL
	40 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8095 mL
	50 mM	0.0579 mL	0.2895 mL	0.5790 mL	1.4476 mL
	60 mM	0.0483 mL	0.2413 mL	0.4825 mL	1.2063 mL
	80 mM	0.0362 mL	0.1810 mL	0.3619 mL	0.9048 mL
	100 mM	0.0290 mL	0.1448 mL	0.2895 mL	0.7238 mL

Vonoprazan Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Vonoprazan (Synonyms: TAK-438 free base)

Customer Review

Other Forms of Vonoprazan:

Vonoprazan Related Antibodies

5 Publications Citing Use of MCE Vonoprazan

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Vonoprazan Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vonoprazan Related Classifications

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