Lynestrenol
产品说明书
 |
同义名 : | Ethinylestrenol |
| CAS号 : | 52-76-6 | |
| 货号 : | A254441 | |
| 分子式 : | C20H28O | |
| 纯度 : | 99% | |
| 分子量 : | 284.44 | |
| MDL号 : | MFCD00051135 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Lynestrenol is used primarily as a component of contraceptive tablets. It has also been used (in combination with mestranol) to control dysfunctional uterine bleeding and endometriosis. Lynestrenol has been tested in mice and rats by oral administration either alone or in combination with mestranol. No increases in any tumor incidences were found. No case reports or human epidemiological studies on lynestrenol alone are available[1]. Fluconazole modestly inhibited both lynestrenol bioactivation and norethindrone biotransformation. Lynestrenol bioactivation was mainly catalysed by recombinant human CYP2C9, CYP2C19 and CYP3A4; rCYP3A4 was responsible for the hydroxylation of norethindrone. The greatest immunoinhibition of lynestrenol bioactivation was seen in incubations with CYP2C-Ab. The CYP3A4-Ab reduced norethindrone hydroxylation by 96%. Both lynestrenol and norethindrone were weak inhibitors of CYP2C9 (IC50 of 32 mM and 46 mM for tolbutamide hydroxylation, respectively)[2]. The treatment of endometriosis with danazol or lynestrenol decreased cholesterol content of plasma high-density lipoproteins by 50% and 32%. There were simultaneous increases in low-density lipoprotein cholesterol content of 51% and 19%[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.52mL 0.70mL 0.35mL |
17.58mL 3.52mL 1.76mL |
35.16mL 7.03mL 3.52mL |
| 参考文献 |
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[1]Lynoestrenol. IARC Monogr Eval Carcinog Risk Chem Hum. 1979 Dec;21:407-15 |