SCH28080

SKU: orb1220157

Description

SCH28080 is a reversible, K+-competitive inhibitor of the gastric (H+/K+)-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.

Key Properties

• CAS Number: 76081-98-6
• MW: 277.32
• Purity: >98% (HPLC)
• Formula: C??H??N?O
• SMILES: N#CCC1=C(C)N=C2C(OCC3=CC=CC=C3)=CC=CN21
• Target: Proton Pump
• Solubility: In Vitro: DMSO : 100 mg/mL (360.59 mM)

Bioactivity

• In Vivo:
  SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats. Animal model: Male Wistar rat (280-350 g), the Shay rat model. Dosage: 20 mg/kg. Administration: Intraperitoneal injection. Result: Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.
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• In Vitro:
  SCH28080 competitively inhibits the K+-stimulated hydrolysis of ATP, with a Ki of 0.12 μM. SCH28080 inhibits histamine-induced [14C]aminopyrine uptake into isolated rabbit parietalcells with an IC50 of 0.029 μM. SCH28080 causes a dose-dependent reduction in cell viability with IC50 values of 22.9 μM and 15.3 μM after 2 h and 24 h treatments, respectively, and cell viability was below 10% at 100 μM already after 2 h treatment. SCH28080 induces apoptosis and is cytotoxic at higher doses. SCH28080 inhibits insulin secretion by activation of IK ATP and inhibition of L-type voltage-gated Ca2+ channels, reduces cell viability and dose-dependently induces apoptosis/necrosis. Cell Viability Assay Cell line: INS-1E cell. Concentration: 3.1 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM Incubation time: 2 hours, 24 hours. Result: Caused a dose-dependent reduction in cell viability.
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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

Quick Database Links

Gene Symbol

Proton Pump