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SCH28080
CAS No. 76081-98-6
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 | ￥907 | 有现货 |
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| 10MG | ￥1337 | 有现货 |
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| 25MG | ￥2260 | 有现货 |
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| 50MG | ￥3370 | 有现货 |
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| 100MG | ￥4803 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称SCH28080
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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
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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。
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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.
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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.
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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.
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同义词——
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通路Membrane Transporter/Ion Channel
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靶点Proton Pump
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受体Ki: 0.12μM ((H+/K+)-ATPase)
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研究领域——
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适应症——
化学信息
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CAS Number76081-98-6
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分子量277.32
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分子式C??H??N?O
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 100 mg/mL (360.59 mM)
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SMILESN#CCC1=C(C)N=C2C(OCC3=CC=CC=C3)=CC=CN21
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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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.
