(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380[1].
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) shows a inhibitory effect in T-47D cells with an IC50 value of 0.110 nM[1]. Cell Viability Assay[1] Cell Line: T-47D cells
(Rac)-Acolbifene (orally adminstration; 7.5 nM, 75 nM; 9 days; once daily) shows a good pharmacological profile in ovariectomized mice, shows 63% and 84% antiuterotrophic inhibitions at the 7.5 and 75 nM doses, respectively (PK study, ovariectomized mice)[1].
[1]. Gauthier S1,et al.Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution.J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77.