存貯條件 | 儲存溫度-20°C |
應(yīng)用 | Letrozole has been used:· in organoid growth assay to determine its inhibitory capacity(48)· to investigate steroid receptor coactivator-1 (SRC-1) mediated endogenous estrogen regulation of hippocampal PSD-95(49)· to determine its effects on tumor-induced hyperalgesia(50)· for hormonal manipulation in rats(51)· to study its effects on lipocalin-2 (Lcn2)(52)· to determine its effects on mechanical hyperalgesia and aromatase expression(53) |
產(chǎn)品介紹 | Letrozole是非甾體類芳香酶抑制劑,其 IC50 為1-13 nM;是第三代aromatase抑制劑,無細胞試驗中IC50為0.07-20 nM。在臨床研究中,對17α-OH progesterone、TSH、促黃體激素、促卵泡激素或雄烯二酮的血漿濃度沒有作用,不影響正常的尿電解質(zhì)排泄或甲狀腺功能。 |
生化機理 | Letrozole acts as an adjuvant agent and is used to treat breast cancer. Letrozole is a third generation nonsteroidal aromatase inhibitor. It is a competitive inhibitor of the aromatase enzyme system and thus inhibits the conversion of androgens to estrogens. Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues. |
別名 | 來曲唑;Femara, Piroxicam; 4,4′-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile |