SRT 1720 is a selective activator of human SIRT1 with an EC 1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC 1.5 s of 37 μM and > 300 μM, respectively.
性状
Solid
IC50 & Target[1][2]
SIRT1 0.16 μM (EC1.5) SIRT2 37 μM (EC1.5)
体外研究(In Vitro)
SRT 1720 effectively decreases the acetylation of p53 in cells even in the absence of SIRT1, and this is attributed to inhibition of histone acetyltransferase p300. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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 Lep 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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 agai
溶解度数据
In Vitro: DMSO : 41.67 mg/mL (88.74 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)配制储备液