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SRT 1720 monohydrochloride is a selective and orally active activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3[1]. | [in vivo]
SRT 1720 (10, 30, 100 mg/kg, p.o.) treatment significantly reduces fasting blood glucose to near normal levels in Lepob/ob mice[1]. 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[2]. 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[3]. | [IC 50]
SIRT1: 0.10 μM (EC50); SIRT1: 0.16 μM (EC1.5); SIRT2: 37 μM (EC1.5) | [References]
[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 DOI:10.1038/nature06261
[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 DOI:10.1038/nrd3738
[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. DOI:10.1172/JCI60132
[4] 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. DOI:10.1161/HYPERTENSIONAHA.116.07709
[5] Lahusen TJ, et al. SRT1720 induces lysosomal-dependent cell death of breast cancer cells. Mol Cancer Ther. 2015 Jan;14(1):183-92. DOI:10.1158/1535-7163.MCT-14-0584 |
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