ACOLBIFENE;EM652
ACOLBIFENE;EM652 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（最大浓度 mg/mL）；109.28（最大浓度 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.70±0.40(Predicted) |
| 颜色 | 白至粉红 |
ACOLBIFENE;EM652 用途与合成方法
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Estrogen receptor 0.110 nM (IC 50 , T-47D cells) |
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.
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. |
