| 应用 |
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) |
| 产品介绍 |
Letrozole是非甾体类芳香酶抑制剂，其 IC50 为1-13 nM；是第三代aromatase抑制剂，无细胞试验中IC50为0.07-20 nM。在临床研究中，对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用，不影响正常的尿电解质排泄或甲状腺功能。 |
| 生化机理 |
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. |
| 别名 |
来曲唑
;Femara, Piroxicam； 4,4′-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile |
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