Acolbifene

Research use only, not for human use.

Acolbifene is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.

Acolbifene is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.(In Vitro):Acolbifene supports the involvement of the clearance-related receptors in its hypocholesterolemic action without affecting pathways of cholesterol synthesis. Acolbifene inhibits estradiol-stimulated cell proliferation in human breast cancer cancer cells including ZR-75-1, MCF-7 and T-47D.(In Vivo):In female Sprague-Dawley rats, Acolbifene (2.5 mg/kg; gavage) reduces food intake, strongly decreases cholesterolemia and prevents tumor growth. Acolbifene reduces food intake (16%) and weight gain (45%, mainly fat).

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.

EM-652

Endocrinology/Hormones

Estrogen Receptor/ERR

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182167-02-8

457.56

C29H31NO4

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (109.28 mM)

CC1=C([C@@H](OC=2C1=CC=C(O)C2)C3=CC=C(OCCN4CCCCC4)C=C3)C5=CC=C(O)C=C5

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(-20℃)

With Ice Pack

≥ 2 years