| 产品描述： | UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively. |
| 靶点： |
IC50: <10 nM (EZH2), 45 nM (EZH1);HistoneMethyltransferase; Autophagy |
| 体内研究： |
A single intraperitoneal (IP) injection of UNC1999 at 15, 50, or 150 mg/kg achieved high Cmax (9,700-11,800 nM) and exhibited dose linearity in male Swiss albino mice. Both the 150 and 50 mg/kg IP doses resulted in the plasma concentrations of UNC1999 above its cellular IC50 over the entire 24 h period while the 15 mg/kg IP dose led to the plasma concentrations of UNC1999 above its cellular IC50 for approximately 12 h. We next examined whether UNC1999 is orally bioavailable and are pleased to find that a single 50 mg/kg oral dose of UNC1999 achieved high Cmax (4,700 nM) and good exposure levels in male Swiss albino mice. The plasma concentrations of UNC1999 are maintained above its cellular IC50 for approximately 20 h following this single oral dose. It is worth noting that all doses including the 150 mg/kg IP dose are well tolerated by all test mice, and no adverse effects are observed |
| 参考文献： |
1. Konze KD, et al. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. |
| 溶解性： |
DMSO : 100 mg/mL (175.52 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.755 ml |
8.776 ml |
17.552 ml |
| 5 mM |
0.351 ml |
1.755 ml |
3.51 ml |
| 10 mM |
0.176 ml |
0.878 ml |
1.755 ml |
| 50 mM |
0.035 ml |
0.176 ml |
0.351 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