SCH28080 ( —— )

产品货号. M21900 CAS No. 76081-98-6

SCH28080 是一种可逆的 K+ 竞争性胃 (H+/K+)-ATP 酶抑制剂，Ki 为 0.12 μM。 SCH28080 是一种有效的体内酸分泌抑制剂，具有抗胃溃疡活性。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥847	有现货
10MG	￥1416	有现货
25MG	￥2344	有现货
50MG	￥3432	有现货
100MG	￥4761	有现货
200MG	￥6507	有现货
500MG	获取报价	有现货
1G	获取报价	有现货
1 mL x 10 mM in DMSO	￥777	有现货

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生物学信息

产品名称

SCH28080
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

SCH28080 是一种可逆的 K+ 竞争性胃 (H+/K+)-ATP 酶抑制剂，Ki 为 0.12 μM。 SCH28080 是一种有效的体内酸分泌抑制剂，具有抗胃溃疡活性。
产品描述

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.
体外实验

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.
体内实验

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 modelDosage:20 mg/kg Administration:Intraperitoneal injection Result:Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.
同义词

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通路

Membrane Transporter/Ion Channel
靶点

Proton Pump
受体

Ki: 0.12μM ((H+/K+)-ATPase)
研究领域

——
适应症

——

化学信息

CAS Number

76081-98-6
分子量

277.32
分子式

C??H??N?O
纯度

>98% (HPLC)
溶解度

In Vitro:?DMSO : 100 mg/mL (360.59 mM)
SMILES

N#CCC1=C(C)N=C2C(OCC3=CC=CC=C3)=CC=CN21
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

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.

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