|4-氧代-6-((嘧啶-2-基硫基)甲基)-4H-吡喃-3-基 4-硝基苯甲酸酯|CsnPharm

CAS No.: 877636-42-5

4-Oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate Catalog No. CSN21287

Synonyms: ML221

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.

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生物活性

实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5950 mL
- 12.9752 mL
- 25.9504 mL
- 5 mM
- 0.5190 mL
- 2.5950 mL
- 5.1901 mL
- 10 mM
- 0.2595 mL
- 1.2975 mL
- 2.5950 mL

技术信息

CAS号

877636-42-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H11N3O6S

运输

蓝冰

分子量

385.35

别名

ML221

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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4-Oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate Catalog No. CSN21287

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