| 产品描述: | AZ876是一种新型的Liver X Receptor (LXR)高亲和力激动剂,对人源LXRα和LXRβ的Ki值分别为0.007 μM和0.011 μM |
| 靶点: |
LXRα:0.007 μM(Ki); LXRβ:0.011 μM(Ki);LiverXReceptor |
| 体外研究: |
In binding assays, AZ876 is 25-fold and 2.5-fold more potent than GW3965 on human (h)LXRα and hLXRβ respectively. In reporter transactivation assays, AZ876 is 196-fold and fivefold more potent than GW3965 on hLXRα and hLXRβ respectively. AZ876 is also more potent than GW3965 on mouse (m)LXRα (248-fold) and mLXRβ (10.5-fold). AZ876 is four- to sevenfold more potent than GW3965 on the expression of ABCA1 mRNA in hamster and human blood PMN cells. AZ876 is highly selective with respect to other nuclear hormone receptors, including retinoid X receptor, farnesoid X receptor, thyroid hormone receptor (TR)α or TRβ, when tested in agonist mode in fluorescence resonance energy transfer assays |
| 体内研究: |
AZ876 is a dual partial LXR agonist that has been shown to reduce atherosclerosis in mice without affecting liver or plasma triglyceride levels when administered in low dose. Chronic administration of the LXR agonist AZ876 attenuates pathological cardiac hypertrophy in a murine model of chronic pressure overload without altering systemic blood pressure, implicating heart-specific effects. AZ876 treatment diminishes myocardial fibrosis and suppresses induction of profibrotic gene expression |
| 参考文献: |
1. JWA van der Hoorn, et al. Low dose of the liver X receptor agonist, AZ876, reduces atherosclerosis in APOE*3Leiden mice without affecting liver or plasma triglyceride levels. Br J Pharmacol. 2011, 162(7): 1553-1563. 2. Cannon MV, et al. The liver X receptor agonist AZ876 protects against pathological cardiac hypertrophy and fibrosis without lipogenic side effects. Eur J Heart Fail. 2015, 17(3):273-82. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.275 ml |
11.375 ml |
22.749 ml |
| 5 mM |
0.455 ml |
2.275 ml |
4.55 ml |
| 10 mM |
0.227 ml |
1.137 ml |
2.275 ml |
| 50 mM |
0.045 ml |
0.227 ml |
0.455 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。 |