Acolbifene|182167-02-8|(EM-652; SCH 57068)-陌孚医药/Medlife

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Acolbifene (Synonyms: EM-652; SCH 57068)

目录号: PL04581 纯度: ≥98%

CAS No. :182167-02-8

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中文名称	Acolbifene
中文别名	3-联苯基溴化镁, 0.5 M 四氢呋喃溶液, J&Kseal瓶;阿考比芬
英文名称	Acolbifene
英文别名	Acolbifene;(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-{4-[2-(1-piperidinyl)ethoxy]p henyl}-2H-chromen-7-ol hydrochloride (1:1);EM652;(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol;Sch 57068;Em-652;Acolbifene (EM 652, SCH57068);(S)-3-(4-hydroxyphenyl)-4-Methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol;2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-(4-(2-(1-piperidinyl)ethoxy)phenyl)-, (S)-;( )-(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2H-1-benzopyran-7-ol
Cas No.	182167-02-8
分子式	C₂₉H₃₂ClNO₄
分子量	494.02
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC 50 = 2 nM) and ERβ (IC 50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.

性状

Solid

IC50 & Target[1][2]

ERα 2 nM (IC50, E2-induced transcriptional activity) ERβ

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.
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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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

ClinicalTrial

参考文献

[1]. Wang T, et al. Recent advances in selective estrogen receptor modulators for breast cancer. Mini Rev Med Chem. 2009 Sep;9(10):1191-201.
[2]. Christian Lemieux, et al. The selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats. J Nutr. 2005 Sep;135(9):2225-9.

溶解度数据	In Vitro: DMSO : 50 mg/mL (109.28 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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