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 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 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 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. 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
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Acolbifene hydrochloride
CAS number：252555-01-4 molecular formula：C29H32ClNO4
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| Chinese alias | 盐酸阿考比芬 | ||
| English alias | (2S)-3-(4-HYDROXYPHENYL)-4-METHYL-2-(4-(2-PIPERIDIN-1-YLETHOXY)PHENYL)-2H-CHROMEN-7-OL, HYDROCHLORIDE | AKOS040745472 | 2H-1-Benzopyran-7-ol,3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-,hydrochloride (1:1), (2S)- | Q27282480 | SCH57 | ||
| CAS number | 252555-01-4 | molecular formula | C29H32ClNO4 |
| molecular weight | 494.02 g/mol | Exact mass | ≥98% |
| PSA | 62.200 Ų | logp | - |
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