ACOLBIFENE;EM652

生物活性靶点体外研究体内研究

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

ACOLBIFENE;EM652化学性质

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)

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。
靶点

Estrogen receptor

0.110 nM (IC ₅₀ , T-47D cells)
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.

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.