中文名称: | Acolbifene | ||||
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英文名称: | Acolbifene | ||||
别名: | Acolbifene EM-652; SCH 57068 | ||||
CAS No: | 182167-02-8 | 分子式: | C29H31NO4 | 分子量: | 457.56074 |
CAS No: | 182167-02-8 | ||||
分子式: | C29H31NO4 | ||||
分子量: | 457.56074 |
基本信息
产品编号: |
A12642 |
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产品名称: |
Acolbifene |
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CAS: |
182167-02-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
457.56 |
-20℃ |
一个月 |
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化学名: |
(S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2H-chromen-7-ol |
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Solubility (25°C): |
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体外:
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DMSO |
50mg/mL(109.28mM;Need ultrasonic) |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.1855mL |
10.9275mL |
21.8551mL |
5mM |
0.4371mL |
2.1855mL |
4.3710mL |
10mM |
0.2186mL |
1.0928mL |
2.1855mL |
生物活性
产品描述 |
EM800 的活性代谢物,是具有口服活性的纯抗雌激素和选择性的雌激素受体 (ER) 的拮抗剂。Acolbifene (EM-652) 抑制雌二醇诱导的 ERα (IC50 = 2nM) 和 ERβ (IC50 = 0.4nM) 转录活性。Acolbifene (EM-652) 具有抗癌活性。 |
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靶点 |
ERα 2nM (IC50, E2-induced transcriptional activity) |
ERβ 0.4nM (IC50, E2-induced transcriptional activity) |
体外研究 |
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 cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity |
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体内研究 |
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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Animal Model: |
Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g. |
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Dosage: |
2.5mg/kg. |
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Administration: |
Oral gavage, once daily for 21 d. |
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Result: |
Prevents tumor growth in rats. |
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 )