产品说明书

ML221

Print
Chemical Structure| 877636-42-5 同义名 : -
CAS号 : 877636-42-5
货号 : A564295
分子式 : C17H11N3O6S
纯度 : 97%
分子量 : 385.351
MDL号 : MFCD06407006
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(77.85 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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

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

[1]Tatemoto K, Hosoya M, Habata Y, et al. Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor. Biochem Biophys Res Commun. 1998;251(2):471‐476.

[2]Maloney PR, Khan P, Hedrick M, et al. Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor. Bioorg Med Chem Lett. 2012;22(21):6656‐6660. doi:10.1016/j.bmcl.2012.08.105

[3]Hall C, Ehrlich L, Venter J, et al. Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth. Cancer Lett. 2017;386:179‐188. doi:10.1016/j.canlet.2016.11.025