(Rac)-Acolbifene (Synonyms: EM-343; (Rac)-EM-652) |
| カタログ番号GC61488 |
(Rac)-アコルビフェン (EM-343; (Rac)-EM-652) は、EM652 (エストロゲン受容体拮抗薬) のラセミ体であり、抗エストロゲン作用とエストロゲン作用を持っています。 (Rac)-アコルビフェン (EM-343; (Rac)-EM-652) はピペリジン環を含み、良好な薬理学的プロファイル、相対結合親和性 (RBA) = 380 を示します。
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Cas No.: 151533-34-5
Sample solution is provided at 25 µL, 10mM.
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(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.
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