Chemistry:ERB-79

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Short description: Chemical compound
ERB-79
Clinical data
Drug classEstrogen; Selective ERβ agonist
Identifiers
CAS Number

ERB-79 is a synthetic estrogen and a selective agonist of the ERβ.[1][2][3] 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

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "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. 2010. doi:10.1186/ar3032. PMID 20497523. 
  2. ↑ 2.0 2.1 "Opposing roles of ERα and ERβ in the genesis and progression of adenocarcinoma in the rat ventral prostate". Prostate 72 (9): 1013–22. 2012. doi:10.1002/pros.21507. PMID 22025007. 
  3. ↑ "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. 2008. doi:10.1210/en.2007-1540. PMID 18174277. 





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