| 产品描述: | BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ |
| 靶点: |
IC50: 68 nM (LXRα); 14 nM (LXRβ);LiverXReceptor |
| 体外研究: |
The LXR selective partial agonist BMS-779788 is identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2 μM, 55% efficacy) |
| 体内研究: |
BMS-779788 induces LXR target genes in blood in vivo with an EC50=610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 is 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B. In mice BMS-779788 displays peripheral induction of ABCA1 at 3 and 10 mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist |
| 参考文献: |
1. Kirchgessner TG, et al. Pharmacological characterization of a novel liver X receptor agonist with partial LXRα activity and a favorable window in nonhuman primates. J Pharmacol Exp Ther. 2015 Feb;352(2):305-14. 2. Kick E, et al. Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ. Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.964 ml |
9.822 ml |
19.644 ml |
| 5 mM |
0.393 ml |
1.964 ml |
3.929 ml |
| 10 mM |
0.196 ml |
0.982 ml |
1.964 ml |
| 50 mM |
0.039 ml |
0.196 ml |
0.393 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。 |