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Vonoprazan Fumarate
CAS No. 881681-01-2
Vonoprazan Fumarate( TAK-438 | TAK 438 | TAK438 | Vonoprazan Fumurate )
Catalog No. M27383 CAS No. 881681-01-2
Vonoprazan Fumurate, a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumurate inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 100MG | 37 | In Stock |
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| 200MG | 59 | In Stock |
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| 500MG | 127 | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameVonoprazan Fumarate
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NoteResearch use only, not for human use.
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Brief DescriptionVonoprazan Fumurate, a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumurate inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.
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DescriptionVonoprazan Fumurate, a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumurate inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.(In Vitro):The inhibitory activity of Vonoprazan Fumurate was unaffected by ambient pH. The inhibition by Vonoprazan Fumurate was reversible and achieved in a K(+)-competitive manner, quite different from that by lansoprazole. Vonoprazan Fumurate exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner.(In Vivo):Vonoprazan Fumurate, at a dose of 4 mg/kg (as the free base) orally, completely inhibited basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats, and its effect on both was stronger than that of lansoprazole. Vonoprazan Fumurate increased the pH of gastric perfusate to a higher value than did lansoprazole or SCH28080, and the effect of Vonoprazan Fumurate was sustained longer than that of lansoprazole or SCH28080.
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In VitroVonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner.Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity.
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In VivoVonoprazan (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 Dosage:0.5, 1, 2, and 4 mg/kg.Administration:Oral administration Result:Inhibited basal gastric acid secretion in a dose-dependent manner.
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SynonymsTAK-438 | TAK 438 | TAK438 | Vonoprazan Fumurate
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PathwayMembrane Transporter/Ion Channel
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TargetProton Pump
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RecptorAntiviral
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Research Area——
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Indication——
Chemical Information
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CAS Number881681-01-2
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Formula Weight461.46
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Molecular FormulaC21H20FN3O6S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 50 mg/mL (108.35 mM)
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SMILESOC(=O)\C=C\C(O)=O.CNCc1cc(-c2ccccc2F)n(c1)S(=O)(=O)c1cccnc1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Yu W, Goddard C, Clearfield E, Mills C, Xiao T, Guo H, Morrey JD, Motter NE, Zhao K, Block TM, Cuconati A, Xu X. Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion. J Med Chem. 2011 Aug 25;54(16):5660-70. doi: 10.1021/jm200696v. Epub 2011 Aug 2. PubMed PMID: 21786803; PubMed Central PMCID: PMC3158247.
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