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) |
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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].
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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. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(109.28 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1855 mL | 10.9275 mL | 21.8551 mL | | 5 mM | 0.4371 mL | 2.1855 mL | 4.3710 mL | | 10 mM | 0.2186 mL | 1.0928 mL | 2.1855 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。 |
