Arzoxifene hydrochloride  

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包装规格:100mg in glass bottle
产品描述:基本信息 产品编号: A12646 产品名称: Arzoxifene hydrochloride CAS: 182133-27-3   储存条件 粉末 -20℃ 四年     分子式: C28H30ClNO4S 溶于液体     分子量 512.06     化学名:  2-(p-Methoxyphenyl)-3-(p-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(b)thiophene-6-ol hydrochloride   生物活性 产品描述 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。 靶点 Estrogen receptor 体外研究 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 体内研究 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 0.01mg/kg with maximal efficacy observed at 0.1-1mg/kg/day. Arzoxifene (LY353381.HCl) antagonizes the estrogen-induced elevation in uterine weight down to vehicle-dosed control levels with ED50 of 0.03mg/kg/day   推荐实验方法(仅供参考) Cell Assay For growth experiments, MCF-7 and MDA-MB-231 cells are treated with Arzoxifene HCl (LY353381.HCl) (0.1, 1, 10, 100, 1000nM). Medium is renewed at days 3 and 5. At day 6, four wells are used for each cell-number determination by counting in a hemocytometer Animal Administration Rats Antiestrogen activity is evaluated in 21-day old Sprague Dawley rats.17α-Ethynyl estradiol at 0.1mg/kg/day is used as the estrogenic stimulus to increase uterine weight in these rats. Arzoxifene HCl (LY353381.HCl)LY353381.HCl (0.001-10mg/kg) or raloxifene (1mg/kg) are administered by oral gavage in a volume of 0.2mL, 15 min prior to the EE2 gavage. Dosing with test compounds is continued for 3 consecutive days. Animals are fasted over night, following the final dose
保存条件:-20℃