| 中文名称: | Arzoxifene hydrochloride | ||||
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| 英文名称: | Arzoxifene hydrochloride | ||||
| 别名: | LY 353381 HCl; SERM 3 | ||||
| CAS No: | 182133-27-3 | 分子式: | C28H30ClNO4S | 分子量: | 512.06 |
| CAS No: | 182133-27-3 | ||||
| 分子式: | C28H30ClNO4S | ||||
| 分子量: | 512.06 | ||||
基本信息
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产品编号： |
A12646 |
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产品名称： |
Arzoxifene hydrochloride |
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CAS: |
182133-27-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
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分子量 |
512.06 |
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化学名： |
2-(p-Methoxyphenyl)-3-(p-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(b)thiophene-6-ol hydrochloride |
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生物活性
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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。 |
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靶点 |
Estrogen receptor |
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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 |
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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)
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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 |
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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 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
