| Description | SCH28080 is a reversible and K+-competitive inhibitor of gastric H+/K+-ATPase with an IC50 value of 20 nM (rabbit microsomal membrane).SCH28080 is a potent inhibitor of acid secretion in vivo with anti-ulcer activity, anti-secretory and cytoprotective activity. |
| In vitro | SCH28080 competitively hinders ATP hydrolysis stimulated by K+, with a Ki value of 0.12 μM.[1]SCH28080 effectively suppresses histamine-induced uptake of [14C]aminopyrine in isolated rabbit parietal cells, demonstrating an IC50 of 0.029 μM.[1]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.[2]SCH28080 induces apoptosis and exhibits cytotoxicity at higher doses.[2].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.[2] |
| In vivo | SCH28080 (20 mg/kg; i.p.) effectively attenuates gastric ulcers induced by pylorus ligation in rats.[3] |
| Target activity | H+, K+-ATPase, rabbit microsomal membranes:20 nM, H+, K+-ATPase:0.12 μM(Ki), Aminopyrine:0.029 μM, INS-1E cells:22.9 µM, INS-1E cells:15.3 µM |
| molecular weight | 277.32 |
| Molecular formula | C17H15N3O |
| CAS | 76081-98-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90.0 mg/mL (324.5 mM), Sonication is recommended. |
| References | 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;36(1):97-104. 2. Jakab M, 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. Hamagishi Y, 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;55(2):283-286. 4. Long JF, et al. Gastric antisecretory and cytoprotective activities of SCH 28080. J Pharmacol Exp Ther. 1983;226(1):114-120. |