CMP8 

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].

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 C_max of 0.5 µM after 30 min^[1][2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

528.08

C₃₃H₃₄ClNO₃

851107-28-3

O=C1CCC2(CC3=CC=C(Cl)C=C3)CC4=C(C=CC(O)=C4)C2=C1C5=CC=C(OCCN6CCCCC6)C=C5

Room temperature in continental US; may vary elsewhere.

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

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

  [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.  [Content Brief]