182167-02-8
182167-02-8 结构式
基本信息
Em 652
CS-1409
Sch 57068
ACOLBIFENE
EM652
Acolbifene (EM 652, SCH57068)
EM652
EM-652
SCH-57068
SCH 57068
EM 652
EM-652
EM652
SCH57068
SCH-57068
SCH 57068.
(S)-3-(4-hydroxyphenyl)-4-Methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
物理化学性质
常见问题列表
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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. |