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ML 221
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML 221图片
CAS NO:877636-42-5
规格:98%
分子量:385.35
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Apelin receptor (APJ) antagonist
CAS:877636-42-5
分子式:C17H11N3O6S
分子量:385.35
纯度:98%
存储:Store at -20°C

Background:

ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.


ML221 is a potent apelin/APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. ML221 is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor (IC50, >79 μM) in cells. ML221 displays limited cross reactivity against a range of GPCRs except the κ-opioid and benzodiazepinone receptors (<50>

参考文献:
[1]. Maloney PR, 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 Nov 1;22(21):6656-60.