ML221

中文名称:

ML221

中文同义词:

化合物ML221

英文名称:

5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one

英文同义词:

5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one;ML221;ML221; ML 221; ML-221;CS-2842;ML 221;ML-221;4H-Pyran-4-one, 5-[(4-nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-;ML221 >=98% (HPLC)

CAS号:

877636-42-5

分子式:

C17H11N3O6S

分子量:

385.35

EINECS号:

相关类别:

API

Mol文件:

877636-42-5.mol

沸点 

624.1±55.0 °C(Predicted)

密度 

1.54±0.1 g/cm3(Predicted)

储存条件 

Sealed in dry,2-8°C

溶解度 

DMSO: soluble5mg/mL, clear (warmed)

形态

powder

酸度系数(pKa)

0.30±0.33(Predicted)

颜色

white to beige

生物活性

ML221 是一种 apelin (APJ) 拮抗剂，抑制 apelin-13 介导的 APJ 的活化，在 cAMP 试验和 β-arrestin 实验中，IC50 值分别为 0.70 μM 和 1.75 μM，EC80 值均为 10 nM。

靶点

IC50: 1.75 μM (APJ, cell-based)

体外研究

ML221 is a potent apelin/APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC 50 s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC 80 of 10 nM in both assays. ML221 is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor (IC 50 , >79 μM) in cells. ML221 displays limited cross reactivity against a range of GPCRs except the κ-opioid and benzodiazepinone receptors (<50/<70%I at 10 μM).

WGK Germany 

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