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

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Acolbifene hydrochloride (Synonyms: EM-652 hydrochloride; SCH 57068 hydrochloride) 纯度: 98.48%

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。

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

Acolbifene hydrochloride Chemical Structure

CAS No. : 252555-01-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2170 In-stock
5 mg ¥2000 In-stock
10 mg ¥3500 In-stock
25 mg ¥6500 In-stock
50 mg ¥9500 In-stock
100 mg ¥13500 In-stock
200 mg   询价  
500 mg   询价  

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Acolbifene hydrochloride 相关产品

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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 (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. 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 cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity[4].

Shanghai Jinpan Biotech Co Ltd 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[2].
Acolbifene (ACOL) reduces food intake (16%) and weight gain (45%, mainly fat) similarly in both dietary cohorts[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

494.02

Formula

C29H32ClNO4

CAS 号

252555-01-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO : 180 mg/mL (364.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0242 mL 10.1210 mL 20.2421 mL
5 mM 0.4048 mL 2.0242 mL 4.0484 mL
10 mM 0.2024 mL 1.0121 mL 2.0242 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (9.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (9.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (9.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
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.

    [3]. A Tremblay, et al. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 1998 Jan;139(1):111-8.

    [4]. Sylvain Gauthier, 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.

    [5]. F Labrie, et al. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium. J Steroid Biochem Mol Biol. Apr-Jun 1999;69(1-6):51-84.

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