rac-Acolbifene

Modify Date: 2024-01-12 11:39:35

rac-Acolbifene Structure
rac-Acolbifene structure
Common Name rac-Acolbifene
CAS Number 151533-34-5 Molecular Weight 457.56100
Density N/A Boiling Point N/A
Molecular Formula C29H31NO4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of rac-Acolbifene


(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].

 Names

Name 2-[4-[2-(1-piperidino)ethoxy]phenyl]-3-(4-hydroxyphenyl)-4-methyl-7-hydroxy-2H-1-benzopyran
Synonym More Synonyms

 rac-Acolbifene 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
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  0

DownStream  1

 Synonyms

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