生物活性 | |||
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描述 | VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces adrenomedullin (AM) production and secretion and downregulates AM receptors on human hepatocytes. VULM 1457 has significant hypolipidemic activity and can improve the overall efficacy of myocardial ischemia-reperfusion injury. VULM 1457 has the potential to study diabetes and hypercholesterolemia [1][2].VULM 1457 significantly down-regulates specific AM receptors on HepG2 cells at concentrations ranging from 0.03 and 0.1 µM and reduces AM secretion in HepG2 cells exposed to hypoxia[1][2].VULM1457 negatively regulates AM-induced cell proliferation[1].Pre-incubation of HepG2 cells with VULM 1457 at a concentration of 0.1 µM significantly reduced the total number of untouched affinity-specific [125I]AM binding found on the cells. Pre-incubation of HepG2 cells with VULM 1457 at high concentrations and at concentrations of 1.0 and 10.0 µM significantly altered AM binding properties[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.22mL 0.44mL 0.22mL |
11.12mL 2.22mL 1.11mL |
22.24mL 4.45mL 2.22mL |
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