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SCH28080 是一种可逆且具有 K+ 竞争性的胃 H+/K+-ATP 酶 (H+/K+-ATPase) 抑制剂,IC50 值为 20 nM (家兔微粒体膜)。SCH28080 在体内是有效的酸分泌抑制剂,具有抗溃疡活性、抗分泌和细胞保护活性。
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SCH28080 是一种可逆且具有 K+ 竞争性的胃 H+/K+-ATP 酶 (H+/K+-ATPase) 抑制剂,IC50 值为 20 nM (家兔微粒体膜)。SCH28080 在体内是有效的酸分泌抑制剂,具有抗溃疡活性、抗分泌和细胞保护活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 328 | 现货 | |
5 mg | ¥ 892 | 现货 | |
10 mg | ¥ 1,490 | 现货 | |
25 mg | ¥ 2,520 | 现货 | |
50 mg | ¥ 3,690 | 现货 | |
100 mg | ¥ 5,290 | 现货 | |
200 mg | ¥ 7,230 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 818 | 现货 |
产品描述 | 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. |
靶点活性 | 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 |
体外活性 | 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] |
体内活性 | SCH28080 (20 mg/kg; i.p.) effectively attenuates gastric ulcers induced by pylorus ligation in rats.[3] |
分子量 | 277.32 |
分子式 | C17H15N3O |
CAS No. | 76081-98-6 |
Smiles | Cc1nc2c(OCc3ccccc3)cccn2c1CC#N |
密度 | 1.16g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 90.0 mg/mL (324.5 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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