Acolbifene (hydrochloride)

252555-01-4

494.02

DMSO : 180 mg/mL (ultrasonic)

Others

Acolbifene (EM-652) hydrochloride, the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) hydrochloride possesses potent and pure anticarcinogenic properties.
In Vitro: 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 ERalpha and ERbeta transcriptional function and blocks the estradiol (E2)-mediated activation of both ERalpha and ERbeta.

Acolbifene (EM-652) shows the most potent inhibition of estradiol-stimulated cell proliferation in human breast cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity.

In Vivo: 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.