SRT1720 | CAS:1001645-58-4

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Name:SRT 1720 Hydrochloride; SRT1720
Cat. No. :CS-0509
CAS No. :1001645-58-4
Formula:C25H24ClN7OS
M. Wt. : 506.02
Solubility:10 mM in DMSO

SRT 1720 Hydrochloride is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.IC50 & Target: EC1.5: 0.16 μM (SIRT1), 37 μM (SIRT2), > 300 μM (SIRT3)[1]In Vitro: SRT1720 and SRT2183 are able to effectively decrease the acetylation of p53 in cells even in the absence of SIRT1, and this is attributed to inhibition of histone acetyltransferase p300[2].In Vivo: SRT1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinaemia after 4 weeks, partially normalizing elevated insulin levels similar to rosiglitazone treatment. SRT1720 treatment significantly reduces fasting blood glucose to near normal levels in Lepob/ob mice[1]. SRT1720 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[2]. SRT1720 (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[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. 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 Gao D, et al. Activation of SIRT1 Attenuates Klotho Deficiency-Induced Arterial Stiffness and Hypertension by Enhancing AMP-Activated Protein Kinase Activity. Hypertension. 2016 Nov;68(5):1191-1199. Baur JA, et al. Are sirtuins viable targets for improving healthspan and lifespan?,Nat Rev Drug Discov. 2012 Jun 1;11(6):443-61