Acolbifene hydrochloride (C09-1101-642)

Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC 50 =2 nM) and ERβ (IC 50 =0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.In VitroAcolbifene (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 cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity . MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAcolbifene (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:Solid. Specifications and Purity: 98%. Molecular Formula: C29H32ClNO4. Molecular Weight: 494.02. PubChem CID: 155436. Isomeric SMILES: CC1=C([C@@H](OC2=C1C=CC(=C2)O)C3=CC=C(C=C3)OCCN4CCCCC4)C5=CC=C(C=C5)O.Cl.