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Vonoprazan hydrochloride

Cat. No. M29058
Vonoprazan hydrochloride Structure
Synonym:

TAK-438 hydrochloride

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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 381.85
Formula C17H17ClFN3O2S
CAS Number 1957202-44-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Feifei Chen, et al. Drug Des Devel Ther. In Vitro and In Vivo Rat Model Assessments of the Effects of Vonoprazan on the Pharmacokinetics of Venlafaxine

[2] Mitsuhiro Nishihara. Eur J Drug Metab Pharmacokinet. Inhibitory Effect of Vonoprazan on the Metabolism of [14C]Prasugrel in Human Liver Microsomes

[3] Takuma Kagami, et al. Clin Pharmacol Ther. Response to "CYP-Mediated Drug-Drug Interaction Is Not a Major Determinant of Attenuation of Antiplatelet Function of Clopidogrel by Vonoprazan"

[4] Mitsuhiro Nishihara, et al. Clin Pharmacol Ther. CYP-Mediated Drug-Drug Interaction Is Not a Major Determinant of Attenuation of Antiplatelet Function of Clopidogrel by Vonoprazan

[5] Takuma Kagami, et al. Clin Pharmacol Ther. Comparative Study of Effects of Vonoprazan and Esomeprazole on Antiplatelet Function of Clopidogrel or Prasugrel in Relation to CYP2C19 Genotype

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Keywords: Vonoprazan hydrochloride, TAK-438 hydrochloride supplier, Proton Pump, inhibitors, activators


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