ACOLBIFENE;EM652
- CAS号:182167-02-8
- 英文名:Sch 57068
- 中文名:ACOLBIFENE;EM652
- CBNumber:CB32495544
- 分子式:C29H31NO4
- 分子量:457.56
- MOL File:182167-02-8.mol
- 沸点 :651.5±55.0 °C(Predicted)
- 密度 :1.217±0.06 g/cm3(Predicted)
- 溶解度 :DMSO:50.0(Max Conc. mg/mL);109.28(Max Conc. mM)
- 形态 :A solid
- 酸度系数(pKa) :9.70±0.40(Predicted)
- 颜色 :White to pink
ACOLBIFENE;EM652性质、用途与生产工艺
- 生物活性 Acolbifene (EM-652) 是 EM800 的活性代谢物，是具有口服活性的纯抗刺激素和选择性的雌激素受体 (ER) 的拮抗剂，其在 T-47D 细胞中的 IC50 值为 0.110 nM。Acolbifene (EM-652) 具有抗癌活性。
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靶点
Estrogen receptor
0.110 nM (IC 50 , T-47D cells)
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体外研究
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.
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体内研究
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.
Animal Model: Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g. Dosage: 2.5 mg/kg. Administration: Oral gavage, once daily for 21 d. Result: Prevents tumor growth in rats.
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
