DCW234 explained
DCW234, also known as butyl 4-(butyryloxy)benzoate, is a synthetic nonsteroidal estrogen and a selective agonist of the ERβ.[1] [2] [3] It shows modest selectivity in terms of affinity and transactivation for the ERβ over the ERα. Its affinity for the ERβ was 3.43 μM and for the ERα was 22.5 μM, while it activated the ERβ and ERα with EC50 values of 1.71–2.5 μM and 19.8–22.5 μM, respectively. As such, its binding selectivity for the ERβ over the ERα was 7-fold and its functional selectivity for the ERβ over the ERα was between 10- and 13-fold.
See also
Notes and References
- Lin Z, Shen H, Huang J, Chen S, Chen L, Chen J, Liu G, Jiang H, Shen X . Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells . J. Steroid Biochem. Mol. Biol. . 110 . 1–2 . 150–6 . 2008 . 18455388 . 10.1016/j.jsbmb.2008.03.028 . 206496235 .
- Minutolo F, Macchia M, Katzenellenbogen BS, Katzenellenbogen JA . Estrogen receptor β ligands: recent advances and biomedical applications . Med Res Rev . 31 . 3 . 364–442 . 2011 . 19967775 . 10.1002/med.20186 . 3841877 .
- Serock MR, Wells AK, Khalil RA . Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause . Recent Pat Cardiovasc Drug Discov . 3 . 3 . 165–86 . 2008 . 18991792 . 10.2174/157489008786263970.
