Name: Vonoprazan fumarate
Price: 498.00 USD

- Overview
  - Vonoprazan fumarate is a pyrole derivative and potassium-competitive acid blocker (P-CAB) that competitively blocks the potassium-binding site of gastric H(+),K(+)-ATPase, a key enzyme in the process of gastric acid secretion.
    
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    Background
    
    Vonoprazan fumarate Inhibits acid secretion by competitively blocking the potassium-binding site of gastric H(+),K(+)-ATPase. The compound can accumulate in acid environments and should provide a longer duration of inhibition due to an alkaline pKa of 9.06. In the presence of acid, this prodrug converts to its active form that covalently binds to certain cysteines in the luminal domain of gastric H(+),K(+)-ATPase.
- Properties
  - CAS Number
    
    1260141-27-2
    
    Molecular Formula
    
    C17H16FN3O2S • C4H4O4
    
    Molecular Weight
    
    461.47
    
    Appearance
    
    White to off-white powder
    
    Solubility
    
    DMSO. Very slightly soluble in water and methanol.
    
    Other Properties
    
    Source: Synthetic
    Purity Level: ≥ 98.5% (by HPLC)
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    Microbiology Applications: Helicobacter pylori (H. pylori) contributes to upper gastrointestinal diseases. Proton pump inhibitor (PPI)-based H. pylori eradication therapy has been shown to be effective for treatment of H. pylori, however, there have been an increase in Clarithromycin resistant strains, thus a more effective strategy is needed. Vonoprazan resulted in a stronger and more sustained acid suppression than PPI-based therapy. (Sakurai et al, 2017).
    
    Eukaryotic Cell Culture Applications: The mode of action of Vonoprazan and Lansoprazole were studied using primary cultured rabbit gastric glands. Both compounds inhibited gastric acid formation in isolated gastric glands (IC₅₀) values, 0.30 and 0.76 μM, respectively. Vonoprazan had a longer and more potent antisecretory effect than Lansoprazole due to its high accumulation and slow clearance from gastric glands (Matsukawa et al, 2011).