rac-Acolbifene
Names
[ CAS No. ]:
151533-34-5
[ 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]:
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C29H31NO4
[ Molecular Weight ]:
457.56100
[ Exact Mass ]:
457.22500
[ PSA ]:
62.16000
[ LogP ]:
5.96480