产品描述: | SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively |
靶点: |
SIRT1:0.16 μM (EC1.5);SIRT2:37 μM (EC1.5);Sirtuin |
体内研究: |
SRT 1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinaemia after 4 weeks, partially normalizing elevated insulin levels similar to rosiglitazone treatment. SRT 1720 treatment significantly reduces fasting blood glucose to near normal levels in Lepob/ob mice. SRT 1720 has ability to protect against the negative effects of diet-induced obesity in mice, and has a connection to metabolic adaptation in fatty acid and oxidative metabolism through downstream targets of SIRT1 such as PGC1α and FOXO1. SRT 1720 (50-100 mg/kg, p.o.), during emphysema development attenuates elastase-induced airspace enlargement and lung function impairment as well as reduces arterial oxygen saturation in WT mice |
参考文献: |
1. Milne JC et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29;450(7170):712-6 2. Baur JA, et al. Are sirtuins viable targets for improving healthspan and lifespan? Nat Rev Drug Discov. 2012 Jun 1;11(6):443-61 3. Yao H, et al. SIRT1 protects against emphysema via FOXO3-mediated reduction of premature senescence in mice. J Clin Invest. 2012 Jun 1;122(6):2032-45. 4. Yu L, et al. Protective effects of SRT1720 via the HNF1α/FXR signalling pathway and anti-inflammatory mechanisms in mice with estrogen-induced cholestatic liver injury. Toxicol Lett. 2016 Dec 15;264:1-11. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.13 ml |
10.648 ml |
21.296 ml |
5 mM |
0.426 ml |
2.13 ml |
4.259 ml |
10 mM |
0.213 ml |
1.065 ml |
2.13 ml |
50 mM |
0.043 ml |
0.213 ml |
0.426 ml |
|
注意: |
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