| Identification | Back Directory | [Name]
9a-(4-chlorobenzyl)-7-hydroxy-4-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one | [CAS]
851107-28-3 | [Synonyms]
CMP8
CMP 8;CMP-8
9a-(4-Chlorobenzyl)-7-hydroxy-4-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-9,9a-dihydro-1H-fluoren-3(2H)-one
9a-(4-chlorobenzyl)-7-hydroxy-4-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one
3H-Fluoren-3-one, 9a-[(4-chlorophenyl)methyl]-1,2,9,9a-tetrahydro-7-hydroxy-4-[4-[2-(1-piperidinyl)ethoxy]phenyl]- | [Molecular Formula]
C33 H34 Cl N O3 | [MOL File]
851107-28-3.mol | [Molecular Weight]
528.08 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [IC 50]
MGERα: 29 nM (IC50); MGRERα: 41 nM (IC50); hERα: 1100 nM (IC50); hERβ: 2200 nM (IC50) | [References]
[1] Miyazaki Y, et al. Destabilizing domains derived from the human estrogen receptor. J Am Chem Soc. 2012 Mar 7;134(9):3942-5. DOI:10.1021/ja209933r
[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. DOI:10.1021/jm060516e |
|
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
|