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ERB-26

ERB-26 is a synthetic estrogen and a selective agonist of the ERβ.^[1][2] It is the active enantiomer of the racemic mixture ERB-79.^[1] Whereas ERB-79 shows 484-fold selectivity for the ERβ over the ERα,^[3] ERB-26 differs slightly in that it is even more selective, showing greater than 1,000-fold selectivity for transactivation of the ERβ relative to the ERα.^[1] Its EC₅₀ value for the ERβ is 0.21 nM (4-fold weaker than estradiol) and for the ERα is 260 nM (10,000-fold weaker than estradiol).^[1] It has no antagonistic activity at either receptor.^[1] ERB-26 is active in prevention of prostate cancer development in preclinical models.^[1] In contrast to ERB-26, the selective ERα agonist ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testosterone alone did not do so.^[1] These findings suggest opposing roles of the ERα and ERβ in the prostate gland.^[1] The chemical structure of ERB-26 does not appear to have been disclosed.

See also[edit]

• Diarylpropionitrile
• ERB-196
• Erteberel
• FERb 033
• Prinaberel (ERB-041)
• WAY-166818
• WAY-200070
• WAY-214156

References[edit]

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