Acolbifene hydrochloride|252555-01-4|(EM-652 hydrochloride; SCH 57068 hydrochloride)-陌孚医药/Medlife

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Acolbifene hydrochloride (Synonyms: EM-652 hydrochloride; SCH 57068 hydrochloride)

目录号: PL04580 纯度: ≥98%

CAS No. :252555-01-4

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中文名称	Acolbifene hydrochloride
英文名称	Acolbifene hydrochloride
英文别名	2H-1-Benzopyran-7-ol,3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-,hydrochloride (1:1), (2S)-;(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2H-chromen-7-ol,hydrochloride;(2S)-3-(4-hydroxyphenyl)-4-methyl-2-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-2H-chromen-7-ol hydrochloride (1:1);Acolbifene hydrochloride;EM-01538;EM-652.HCl;SCH-57068.HCl
Cas No.	252555-01-4
分子式	C₂₉H₃₁NO₄^.HCl
分子量	494.02
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Acolbifene (EM-652) hydrochloride 是 EM800 的活性代谢产物，是一种口服活性的选择性雌激素受体调节剂 (SERM)。Acolbifene (EM-652) hydrochloride 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) hydrochloride 对乳腺和子宫有明显的抗雌激素作用。Acolbifene (EM-652) hydrochloride 具有抗癌活性。

生物活性

Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC 50 =2 nM) and ERβ (IC 50 =0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. 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 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

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 : 180 mg/mL (364.36 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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