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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。
Acolbifene图片
CAS NO:182167-02-8
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
EM-652
SCH 57068
产品介绍
Acolbifene (EM-652) 是 EM800 的活性代谢物，是具有口服活性的纯抗雌激素和选择性的雌激素受体(ER)的拮抗剂。Acolbifene (EM-652) 抑制雌二醇诱导的 ERα (IC50= 2 nM) 和 ERβ (IC50= 0.4 nM) 转录活性。Acolbifene (EM-652) 具有抗癌活性。
生物活性

Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selectiveestrogen receptorantagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity ofERα(IC50= 2 nM) andERβ(IC50= 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties[1][2][3][4][5].

IC50& Target[5]

ERα

2 nM (IC50, E2-induced transcriptional activity)

ERβ

0.4 nM (IC50, E2-induced transcriptional activity)

体外研究
(In Vitro)

Acolbifene (ACOL) does not affect pathways of cholesterol synthesis, supporting the involvement of the clearance-related receptors in its hypocholesterolemic action[2].
Acolbifene (EM-652) shows no agonistic activity on ERα and ERβ transcriptional function and blocks the estradiol (E2)-mediated activation of both ERα and ERβ[3].
Acolbifene (EM-652) shows the most potent inhibition of estradiol-stimulated cell proliferation in human breast cancer cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity[4].

体内研究
(In Vivo)

Acolbifene (ACOL) reduces food intake and strongly decreases cholesterolemia in rats fed a cholesterol-free diet[2].
Acolbifene (ACOL) reduces food intake (16%) and weight gain (45%, mainly fat) similarly in both dietary cohorts[2].

Animal Model:Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g[2].
Dosage:2.5 mg/kg.
Administration:Oral gavage, once daily for 21 d.
Result:Prevents tumor growth in rats.
Clinical Trial
分子量

457.56

性状

Solid

Formula

C29H31NO4

CAS 号

182167-02-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(109.28 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1855 mL10.9275 mL21.8551 mL
5 mM0.4371 mL2.1855 mL4.3710 mL
10 mM0.2186 mL1.0928 mL2.1855 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。