Vonoprazan Fumarate (TAK-438)

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
1g	$150	Check With Us
2g	$245	Check With Us
5g	$390	Check With Us

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Cat #: V1677 CAS #: 1260141-27-2 Purity ≥ 98%

Description: Vonoprazan Fumarate (formerly TAK-438, TAK 438, trade name Takecab), the fumarate salt of Vonoprazan, is a novel, orally bioactive and potent P-CAB (potassium-competitive acid blocker) that has been approved in Janpan in 2015 for the treatment of gastroduodenal ulcer and reflux esophagitis.

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	461.46
Molecular Formula	C17H16FN3O2S.C4H4O4
CAS No.	1260141-27-2
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 62 mg/mL (134.4 mM)r
	Water:<1 mg/mLr
	Ethanol:<1 mg/mL
Solubility In Vivo	0.5% methylcellulose: 17 mg/mL
Synonyms	TAK438, Vonoprazan Fumarate, TAK-438, TAK 438, Takecab

Protocol	In Vitro	Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity
	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
	Animal model	Male 7- or 8-week-old Sprague-Dawley rat
	Dosages	0.5, 1, 2, and 4 mg/kg
	Administration	Oral administration

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.1670 mL	10.8352 mL	21.6704 mL	43.3407 mL
5mM	0.4334 mL	2.1670 mL	4.3341 mL	8.6681 mL
10mM	0.2167 mL	1.0835 mL	2.1670 mL	4.3341 mL
20mM	0.1084 mL	0.5418 mL	1.0835 mL	2.1670 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

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

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.