ML221
产品说明书
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同义名 : | - |
| CAS号 : | 877636-42-5 | |
| 货号 : | A564295 | |
| 分子式 : | C17H11N3O6S | |
| 纯度 : | 97% | |
| 分子量 : | 385.35 | |
| MDL号 : | MFCD06407006 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Apelin, a circulating peptide hormone, is synthesized and secreted by a variety of cell types including those of the cardiovascular, endocrine, gastrointestinal and nervous systems. Apelin was recently identified as the endogenous ligand of the APJ, a formerly orphaned G-protein coupled receptor (GPCR) with a similarly broad distribution of expression[1]. ML221 is a potent apelin receptor (APJ) antagonist with IC50s of 0.70 μM and 1.75 μM in cAMP and β-arrestin assay respectively[2]. Cholangiocarcinoma (CCA) cell line HuH-28 treated with 10 μM of ML221 for 24 h showed significant decreased expression of Ki-67, as well as VEGF-A, VEGF-C, Ang-1 and Ang-2, while these were not observed in SG231 cells. CCA xenograft tumors in mice were treated with ML221 (150 μg/kg) for 3× weekly via tail vein injection for 4 weeks, and tumor volumes were significantly smaller compared to those in the untreated control mice[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.60mL 0.52mL 0.26mL |
12.98mL 2.60mL 1.30mL |
25.95mL 5.19mL 2.60mL |
| 参考文献 |
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