rac-Acolbifene

Names

[ Name ]:
rac-Acolbifene

[Synonym ]:
7-hydroxy-3-(4'-hydroxyphenyl)-4-methyl-2-(4"-(2"'-piperidinoethoxy)phenyl)-2H-benzopyran
rac-Acolbifene
2-[4-[2-(1-piperidino)ethoxy]phenyl]-3-(4-hydroxyphenyl) -4-methyl-7-hydroxy-2H-1-benzopyran

Biological Activity

[Description]:

(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].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

[In Vitro]

(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 Concentration: 0.110 nM Incubation Time: 72 hours Result: Inhibited T-47D cells growth.

[In Vivo]

(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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₁NO₄

[ Molecular Weight ]:
457.56100

[ Exact Mass ]:
457.22500

[ PSA ]:
62.16000

[ LogP ]:
5.96480

Precursor & DownStream

Precursor

DownStream

Related Compounds

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