| 产品描述: | AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with Kds of 1.8 and 3.1 μM, respectively. |
| 靶点: |
Kd: 1.8 μM (AdipoR1), 3.1 μM (AdipoR2);Adiponectinreceptor |
| 体内研究: |
AdipoRon (50 mg/kg, i.v.) cuases significant phosphorylation of AMPK in skeletal muscle and liver of wild-type mice but not Adipor1−/− Adipor2−/− double-knockout mice. AdipoRon (0.02, 0.1, and 0.5 mg/kg, i.g.) alleviates D-GalN induced hepatotoxicity in mice, and prevents hepatic architecture distortion against D-GalN challenge. The hepatoprotective potential of AdipoRon is particularly evident in higher dosages (0.1 and 0.5 mg/kg). Enhanced cardiomyocyte apoptosis in APN-deficient mice is rescued by AdipoRon (50 mg/kg, p.o.) administration. Antiapoptotic effect of AdipoRon is attenuated but not lost in AMPK-DN mice |
| 参考文献: |
1. Okada-Iwabu M, et al. A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Nature. 2013 Nov 28;503(7477):493-9. 2. Wang Y, et al. Hepatoprotective effects of AdipoRon against d-galactosamine-induced liver injury in mice. Eur J Pharm Sci. 2016 Aug 9;93:123-131. 3. Zhang Y, et al. AdipoRon, the first orally active adiponectin receptor activator, attenuates postischemic myocardial apoptosis through both AMPK-mediated and AMPK-independent signalings. Am J Physiol Endocrinol Metab. 2015 Aug 1;309(3):E275-82. 4. Hong K, et al. Adiponectin Receptor Agonist, AdipoRon, Causes Vasorelaxation Predominantly Via a Direct Smooth Muscle Action. Microcirculation. 2016 Apr;23(3):207-20. |
| 溶解性: |
DMSO : 62.5 mg/mL (145.85 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) |
| 保存条件: |
RT |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.334 ml |
11.668 ml |
23.336 ml |
| 5 mM |
0.467 ml |
2.334 ml |
4.667 ml |
| 10 mM |
0.233 ml |
1.167 ml |
2.334 ml |
| 50 mM |
0.047 ml |
0.233 ml |
0.467 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。 |