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(Rac)-Acolbifene
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(Rac)-Acolbifene图片
CAS NO:151533-34-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
(Rac)-Acolbifene(EM-343;(Rac)-EM-652)是EM652(estrogenreceptor拮抗剂)的外消旋形式,具有抗雌激素和雌激素活性。(Rac)-Acolbifene(EM-343;(Rac)-EM-652)含哌啶环,具有良好的药理作用,RBA=380。
Cas No.151533-34-5
别名EM-343; (Rac)-EM-652
Canonical SMILESOC1=CC=C2C(C)=C(C3=CC=C(O)C=C3)C(C4=CC=C(OCCN5CCCCC5)C=C4)OC2=C1
分子式C29H31NO4
分子量457.56
溶解度DMSO: 100 mg/mL (218.55 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

(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.