| 产品描述: | RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research. |
| 体内研究: |
RXR antagonist 1 (compound 6a) shows potent RXR-antagonistic activities at 1 μM. RXR antagonist 1 shows competitive binding to the LBP in hRXRα-LBD, with Ki of 0.384 ± 0.072, Kd of 0.277 ± 0.038, and Ki/Kd of 1.39. The cell permeability of RXR antagonist 1 shows no correlation with RXR-antagonistic activity. |
| 参考文献: |
1. Masaki Watanabe, et al. Increased Molecular Flexibility Widens the Gap between Ki and Kd values in Screening for Retinoid X Receptor Modulators. ACS Med. Chem. Lett. 2022, 13, 2, 211-217. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.99 ml |
9.949 ml |
19.898 ml |
| 5 mM |
0.398 ml |
1.99 ml |
3.98 ml |
| 10 mM |
0.199 ml |
0.995 ml |
1.99 ml |
| 50 mM |
0.04 ml |
0.199 ml |
0.398 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。 |