Vonoprazan Fumarate

SKU: orb1940457

Description

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.(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 881681-01-2
• MW: 461.46
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀FN₃O₆S
• SMILES: OC(=O)\C=C\C(O)=O.CNCc1cc(-c2ccccc2F)n(c1)S(=O)(=O)c1cccnc1
• Target: Proton Pump
• Solubility: In Vitro: DMSO : 50 mg/mL (108.35 mM)

Bioactivity

• 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. 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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• In Vitro:
  Vonoprazan (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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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAK-438 | TAK 438 | TAK438 | Vonoprazan Fumurate

Quick Database Links

Gene Symbol

Proton Pump