SRT 1720

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC_1.5 = 0.16 versus 46.2 ?M, respectively).¹ In diet-induced obese and diabetic leptin-deficient ob/ob mice, oral administration of 100 mg/kg SRT1720 once daily improves insulin sensitivity, lowers plasma glucose and increases mitochondrial capacity after one week of treatment.¹ In Zucker fa/fa rats, SRT 1720 improves whole-body glucose homeostasis and insulin sensitivity in adipose tissue, skeletal muscle, and liver.¹

1.Milne, J.C., Lambert, P.D., Schenk, S., et al.Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetesNature450(7170)712-716(2007)