| Clinical data | |
|---|---|
| Drug class | Estrogen; Selective ERβ agonist |
| Identifiers | |
| CAS Number | |
| PubChem SID | |
ERB-79 is a synthetic estrogen and a selective agonist of the ERβ.123 It is a racemic mixture, with the active enantiomer being ERB-26.2 ERB-79 shows more than 484-fold selectivity for transactivation of the ERβ over the ERα.1 Its EC50 value for the ERβ is 0.448 nM (14.52% of the potency of estradiol) and for the ERα is 79 nM (0.03% of the potency of estradiol).1 It has no antagonistic activity at either receptor.1 ERB-79 is active in preclinical models of arthritis.1 The chemical structure of ERB-79 does not appear to have been disclosed.
See also
See also
References
References
- Dulos J, Vijn P, van Doorn C, Hofstra CL, Veening-Griffioen D, de Graaf J, Dijcks FA, Boots AM (2010). "Suppression of the inflammatory response in experimental arthritis is mediated via estrogen receptor α but not estrogen receptor β". Arthritis Res. Ther. 12 (3) R101. doi:10.1186/ar3032. PMC 2911889. PMID 20497523.
- Attia DM, Ederveen AG (2012). "Opposing roles of ERα and ERβ in the genesis and progression of adenocarcinoma in the rat ventral prostate". Prostate. 72 (9): 1013–22. doi:10.1002/pros.21507. PMID 22025007. S2CID 12951793.
- Roa J, Vigo E, Castellano JM, Gaytan F, Navarro VM, Aguilar E, Dijcks FA, Ederveen AG, Pinilla L, van Noort PI, Tena-Sempere M (2008). "Opposite roles of estrogen receptor (ER)-α and ERβ in the modulation of luteinizing hormone responses to kisspeptin in the female rat: implications for the generation of the preovulatory surge". Endocrinology. 149 (4): 1627–37. doi:10.1210/en.2007-1540. PMID 18174277.