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Arzoxifene hydrochloride

CAS No. : 182133-27-3

MCE 国际站：Arzoxifene hydrochloride

产品活性：Arzoxifene (LY353381) hydrocloride 是一种选择性的雌激素受体 (estrogen receptor) 调节剂，它是乳腺和子宫组织中有效的雌激素拮抗剂，同时作为维持骨密度和降低血清胆固醇的雌激素激动剂。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

In Vitro: Arzoxifene inhibits cell growth as effectively as the antiestrogen tamoxifen. Northern analysis reveals that arzoxifene exerts a statistically significant inhibition of pS2 ａnd progesterone receptor B mRNA expression. Significant agonistic effect is observed on the antitrypsin mRNA expression. In contrast to estradiol ａnd tamoxifen, arzoxifene does not upregulate cathepsin D mRNA ａnd protein expression.

In Vivo: Arzoxifene prevents the ovariectomy-induced increase in body weight ａnd serum cholesterol levels of treated rats ａnd lowers them to below sham levels in a dose dependent manner, with maximum efficacy similar to estrogen or raloxifene. Arzoxifene (LY353381.HCl) prevents loss of bone due to ovariectomy with an ED₅₀ of about 0.01 mg/kg with maximal efficacy observed at 0.1-1 mg/kg/day. Arzoxifene (LY353381.HCl) antagonizes the estrogen-induced elevation in uterine weight down to vehicle-dosed control levels with ED₅₀ of 0.03 mg/kg/day.

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