| 靶点： |
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells. |
| 体外研究： |
Y134 exhibits potent antagonist activity at ERs in CV-1 cells cotransfected with plasmids containing ERα or ERβ and oestrogen-response element-driven luciferase, with IC50. |
| 体内研究： |
Y134 (1-3 mg/kg/day; p.o. for 3 days) abolishes the E2-induced mammary gland terminal end bud (TEB) outgrowth in ovariectomized rats. Y134 inhibits uterine cell proliferation induced by E2 in a dose-dependent manner. |
| 参考文献： |
[1]. Ning M, et, al. Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134). Br J Pharmacol. 2007 Jan;150(1):19-28. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.116 ml |
10.58 ml |
21.16 ml |
| 5 mM |
0.423 ml |
2.116 ml |
4.232 ml |
| 10 mM |
0.212 ml |
1.058 ml |
2.116 ml |
| 50 mM |
0.042 ml |
0.212 ml |
0.423 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京