Acolbifene,252555-01-4

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Acolbifene hydrochloride

CAS No. : 252555-01-4

MCE 国际站：Acolbifene hydrochloride

产品活性：Acolbifene (EM-652) hydrochloride 是 EM800 的活性代谢产物，是一种口服活性的选择性雌激素受体调节剂 (SERM)。Acolbifene (EM-652) hydrochloride 抑制雌二醇诱导的 ERα (IC₅₀ = 2 nM) 和 ERβ (IC₅₀ = 0.4 nM) 转录活性。Acolbifene (EM-652) hydrochloride 对乳腺和子宫有明显的抗雌激素作用。Acolbifene (EM-652) hydrochloride 具有抗癌活性。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

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.

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.

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