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ERB-79

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Chemical compound Pharmaceutical compound
ERB-79
Clinical data
Drug classEstrogen; Selective ERβ agonist
Identifiers
CAS Number
PubChem SID

ERB-79 is a synthetic estrogen and a selective agonist of the ERβ. It is a racemic mixture, with the active enantiomer being ERB-26. ERB-79 shows more than 484-fold selectivity for transactivation of the ERβ over the ERα. 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). It has no antagonistic activity at either receptor. ERB-79 is active in preclinical models of arthritis. The chemical structure of ERB-79 does not appear to have been disclosed.

See also

References

  1. ^ 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.
  2. ^ 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.
  3. 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.


Estrogen receptor modulators
ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
  • Coregulator-binding modulators: ERX-11
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown
See also
Receptor/signaling modulators
Estrogens and antiestrogens
Androgen receptor modulators
Progesterone receptor modulators
List of estrogens


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