| Bioactivity | 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[1][2][3]. | |||||||||
| Target | Ki: 0.12 μM ((H+/K+)-ATPase) | |||||||||
| Invitro | SCH28080 competitively inhibits the K+-stimulated hydrolysis of ATP, with a Ki of 0.12 μM [1].SCH28080 inhibits histamine-induced [14C]aminopyrine uptake into isolated rabbit parietal cells with an IC50 of 0.029 μM[1].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[2].SCH28080 induces apoptosis and is cytotoxic at higher doses[2].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[2]. Cell Viability Assay[2] Cell Line: | |||||||||
| In Vivo | SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats[3]. Animal Model: | |||||||||
| Name | SCH28080 | |||||||||
| CAS | 76081-98-6 | |||||||||
| Formula | C17H15N3O | |||||||||
| Molar Mass | 277.32 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Scott CK, et al. Studies on the mechanism of action of the gastric microsomal (H+ + K+)-ATPase inhibitors SCH 32651 and SCH 28080. Biochem Pharmacol. 1987 Jan 1;36(1):97-104. [2]. Martin Jakab, et al. The H+/K+ ATPase Inhibitor SCH-28080 Inhibits Insulin Secretion and Induces Cell Death in INS-1E Rat Insulinoma Cells. Cell Physiol Biochem. 2017;43(3):1037-1051. [3]. Y Hamagishi, et al. Inhibitory Effects of Copiamycin A, a Macrocyclic Lactone Antibiotic, on Gastric H+,K(+)-ATPase, Acid Secretion and Ulcer Formation. Jpn J Pharmacol. 1991 Feb;55(2):283-6. |