(Rac)-Acolbifene|151533-34-5|(EM-343; (Rac)-EM-652)-陌孚医药/Medlife

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(Rac)-Acolbifene (Synonyms: EM-343; (Rac)-EM-652)

目录号: PL04582 纯度: ≥99%

CAS No. :151533-34-5

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中文名称	(Rac)-Acolbifene
中文别名	4-氨基-N-[(1S)-1-(4-氯苯基)-3-羟基丙基]-1-(7H-吡咯并[2,3-D]嘧啶-4-基)-4-哌啶甲酰胺
英文名称	(Rac)-Acolbifene
英文别名	2H-1-Benzopyran-7-ol,3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-;EM 343;ACOLBIFENE;rac-Acolbifene;2-[4-[2-(1-piperidino)ethoxy]phenyl]-3-(4-hydroxyphenyl)-4-Methyl-7-hydroxy-2H-1-benzopyran;(Rac)-Acolbifene
Cas No.	151533-34-5
分子式	C₂₉H₃₁NO₄
分子量	457.56
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	(Rac)-Acolbifene (EM-343; (Rac)-EM-652) 是 EM652 (estrogen receptor 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。
生物活性	(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.
性状	Crystal
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (218.55 mM; Need ultrasonic)配制储备液

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