AU-461
AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM) . AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers[1].
Product Specifications
CAS Number
[220854-06-8]
UNSPSC
12352005
Target
Na+/K+ ATPase
Related Pathways
Membrane Transporter/Ion Channel
Field of Research
Metabolic Disease
Smiles
CC1=C(N2C3=C(CC2)C(NCCO)=NC4=C3C=CC=C4OCC(F)(F)F)C=CC(OC)=C1
Molecular Formula
C23H24F3N3O3
Molecular Weight
447.45
References & Citations
[1]Cheon HG, et al. Pharmacological properties of the gastric H (+) /K (+) ATPase inhibitor, AU-461. Pharmacology. 2000 Apr;60 (3) :161-8.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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