产品
编 号:F451600
分子式:C17H15N3O
分子量:277.32
产品类型
结构图
CAS No: 76081-98-6
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产品详情
生物活性:
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.
体内研究:
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.
体外研究:
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.