他莫昔芬是一种选择性雌激素反应调节剂（SERM）、蛋白激酶C抑制剂和抗血管生成因子。他莫昔芬是一种前药，可通过细胞色素P450的异构体CYP2D6和CYP3A4代谢成活性代谢产物4-羟基三苯氧胺（4-OHT）和内啡肽。在乳腺癌中，他莫昔芬针对ERBB2的基因阻遏活性依赖于PAX2。在乳腺肿瘤细胞中阻断雌二醇刺激的VEGF的产生。 应用： 他莫昔芬已用于促进ect2flox等位基因在小鼠器官中的重组。它也用于研究其对脂多糖（LPS）诱导的小胶质细胞激活的影响。 Tamoxifen is a selective estrogen response modifier (SERM), protein kinase C inhibitor and anti-angiogenetic factor. Tamoxifen is a prodrug that is metabolized to active metabolites 4-hydroxytamoxifen (4-OHT) and endoxifen by cytochrome P450 isoforms CYP2D6 and CYP3A4. In breast cancer, the gene repressor activity of tamoxifen against ERBB2 is dependent upon PAX2. Blocks estradiol-stimulated VEGF production in breast tumor cells. Tamoxifen has been used to facilitate the recombination of ect2 flox allele in mouse organs 91 . It has also been used to study its effect on lipopolysaccharide (LPS)-induced microglial activation 92 .