CMP8

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CMP8 

CMP8 是雌激素受体 (estrogen receptor) 的选择性配体，可结合到雌激素受体配体结合域。CMP8 对突变型 MGERα、MGRERα 和野生型 hERα、hERβ 的IC50 值分别为 29 nM、41 nM、1100 nM 和2200 nM。

CMP8

CMP8 Chemical Structure

CAS No. : 851107-28-3

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生物活性

CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively[1][2].

IC50 & Target

MGERα

29 nM (IC50)

MGRERα

41 nM (IC50)

hERα

1100 nM (IC50)

hERβ

2200 nM (IC50)

体内研究
(In Vivo)

CMP8 (Compound 20h) is dosed in male Balb-c mice (4 mg/kg, ip). The plasma concentration after 4 h is 1.5-fold its EC50 in mammalian cells with a Cmax of 0.5 µM after 30 min[1][2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

528.08

Formula

C33H34ClNO3
CAS 号

851107-28-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Miyazaki Y, et al. Destabilizing domains derived from the human estrogen receptor. J Am Chem Soc. 2012 Mar 7;134(9):3942-5.

    [2]. Kinzel O, et al. A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies. J Med Chem. 2006 Sep 7;49(18):5404-7.

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