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SCH28080

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Chemical Structure| 76081-98-6 同义名 : -
CAS号 : 76081-98-6
货号 : A1176583
分子式 : C17H15N3O
纯度 : 99%+
分子量 : 277.32
MDL号 : MFCD00834620
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(378.62 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 SCH28080 is a reversible K+-competitive inhibitor of gastric H,K-ATPase with a Ki value of 0.12 μM.SCH28080 is a potent in vivo inhibitor of gastric acid secretion with anti-gastric ulcer activity[1][2][3].SCH28080 inhibits histamine-induced uptake of [14C]aminopyrine in isolated rabbit parietal cells with an IC50 of 0.029 μM[1].SCH28080 resulted in a dose-dependent decrease in cell viability, with IC50 values of 22.9 µM and 15.3 µM after 2 and 24 h of treatment, respectively, and cell viability was already below 10% at 100 µM after 2 h of treatment.SCH28080 inhibited insulin secretion through activation of IK ATP and inhibition of L-type voltage-gated Ca2+ channels, decreased cell viability and dose-dependently induces apoptosis/necrosis and is cytotoxic at higher doses[2] .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.61mL

0.72mL

0.36mL

18.03mL

3.61mL

1.80mL

36.06mL

7.21mL

3.61mL
参考文献

[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.