| 货号 | 13863-50mg |
| 描述 | Estrogen action is mediated through two estrogen receptor (ER) subtypes, ERα and ERβ, which have distinct target tissue distributions and functional activities.1 Methylpiperidino pyrazole is an ER antagonist that is highly selective for ERα compared to ERβ (Kis = 5.6 nM and 2.3 μM, respectively).2 It can inhibit ERα transcriptional activation with an IC50 value of 80 nM.3 It has been used to evaluate the role of ERα in various estrogen-responsive systems, including certain cancers.4 |
| 别名 | MPP; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hall, J.M.,Couse, J.F. and Korach, K.S. The multifaceted mechanisms of estradiol and estrogen receptor signaling. The Journal of Biological Chemisty 276(40), 36869-26872 (2001). 2.Sun, J.,Huang, Y.R.,Harrington, W.R., et al. Antagonists selective for estrogen receptor α. Endocrinology 143(3), 941-947 (2002). 3.Zhou, H.B.,Carlson, K.E.,Stossi, F., et al. Analogs of methyl-piperidinopyrazole (MPP): Antiestrogens with estrogen receptor α selective activity. Bioorganic & Medicinal Chemistry Letters 19(1), 108-110 (2009). 4.Davis, A.M.,Mao, J.,Naz, B., et al. Comparative effects of estradiol, methyl-piperidino-pyrazole, raloxifene, and ICI 182 780 on gene expression in the murine uterus. Journal of Molecular Endocrinology 41, 205-217 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 469.6 |
| 分子式 | C29H31N3O3 |
| CAS号 | 289726-02-9 |
| 稳定性 | ≥ 2 years |
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