SCH28080

SKU: orb1706648

Description

SCH28080 is a reversible, potassium-competitive inhibitor of gastric H+/K+-ATPase, exhibiting potent anti-secretory and cytoprotective effects. With an IC50 of 20 nM in rabbit microsomal assays, it demonstrates significant anti-ulcer activity in vivo, making it a valuable research tool for studying gastric acid secretion and gastrointestinal pharmacology.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 76081-98-6
• MW: 277.32
• Purity: 97.12% (May vary between batches)
• Formula: C₁₇H₁₅N₃O
• SMILES: Cc1nc2c(OCc3ccccc3)cccn2c1CC#N
• Target: ATPase,Proton pump
• Solubility: DMSO:90 mg/mL (324.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (11.9 mM)

Bioactivity

• Target IC50:
  INS-1E cells:22.9 µM|INS-1E cells:15.3 µM|H+, K+-ATPase, rabbit microsomal membranes:20 nM|H+, K+-ATPase:0.12 μM(Ki)|Aminopyrine:0.029 μM
• In Vivo:
  SCH28080 (20 mg/kg; i.p.) effectively reduces gastric ulcers induced by pylorus ligation in rats.
• In Vitro:
  SCH28080 competitively hinders ATP hydrolysis stimulated by K+, with a Ki value of 0.12 μM. SCH28080 effectively suppresses histamine-induced uptake of [14C]aminopyrine in isolated rabbit parietal cells, demonstrating an IC50 of 0.029 μM. SCH28080 elicits a dose-dependent decrease in cell viability, with IC50 values of 22.9 µM and 15.3 µM following 2-hour and 24-hour treatments, respectively. And at concentration of 100 µM, cell viability drops below 10% as early as 2 hours. SCH28080 induces apoptosis and exhibits cytotoxicity at higher doses.. SCH28080 also impedes insulin secretion by activating IK ATP and inhibiting L-type voltage-gated Ca2+ channels, ultimately reducing cell viability and induces apoptosis/necrosis in a dose-dependent manner.
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Storage & Handling

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

Alternative Names

H+/K+-ATPase, H+/K+-ATPase, rabbit microsomal membranes, SCH 28080, SCH28080, SCH-28080, Proton pump, Protonpump

Compound Identifiers

PubChem CID

108137