SRT 1720 didrochloride is a selective and orally active activator of SIRT3[1].
即使在没有 SIRT1 的情况下，SRT 1720 didrochloride 也能有效地降低细胞中 p53 的乙酰化，这归因于组蛋白乙酰转移酶 p300[2]。
SRT 1720 (10, 30, 100 mg/kg, p.o.) didrochloride 处理显著降低 Lepob/ob 小鼠的空腹血糖至接近正常水平[1]。
SRT 1720 didrochloride 能够保护小鼠免受饮食诱导的肥胖的负面影响，并通过 SIRT1 的下游靶点，如 PGC1α 和 FOXO1，与脂肪酸和氧化代谢的代谢适应有关[2]。
SRT 1720 (50-100 mg/kg, p.o.) didrochloride 在肺气肿发展过程中减弱弹性酶诱导的气道扩大和肺功能损害，并降低野生小鼠的动脉氧饱和度[3]。
[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 empsema via FOXO3-mediated reduction of premature senescence in mice.,J Clin Invest. 2012 Jun 1;122(6):2032-45.
[4]. Gao D, et al. Activation of SIRT1 Attenuates Klotho Deficiency-Induced Arterial Stiffness and pertension by Enhancing AMP-Activated Protein Kinase Activity. pertension. 2016 Nov;68(5):1191-1199.
[5]. Lahusen TJ, et al. SRT1720 induces lysosomal-dependent cell death of breast cancer cells. Mol Cancer Ther. 2015 Jan;14(1):183-92.