2. Membrane Transporter/Ion Channel
  3. Na+/K+ ATPase
  4. 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.

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AU-461

AU-461 Chemical Structure

CAS No. : 220854-06-8

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Description

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].

Molecular Weight

447.45

Formula

C23H24F3N3O3
CAS No.
SMILES

CC1=C(N2C3=C(CC2)C(NCCO)=NC4=C3C=CC=C4OCC(F)(F)F)C=CC(OC)=C1
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AU-461 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AU-461220854-06-8AU461AU 461Na+/K+ ATPaseSodium potassium pumpH+/K+ ATPase inhibitorreversible inhibitionantiulcer agentgastric acid secretionplasma gastrincompetitive inhibitionInhibitorinhibitorinhibit

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