2468639-77-0

2468639-77-0 structure
2468639-77-0 structure
  • Name: SRT 1720 dihydrochloride
  • Chemical Name: SRT 1720 dihydrochloride
  • CAS Number: 2468639-77-0
  • Molecular Formula: C25H25Cl2N7OS
  • Molecular Weight: 542.48
  • Catalog: Signaling Pathways Autophagy Autophagy
  • Create Date: 2023-05-22 17:26:29
  • Modify Date: 2024-04-02 20:08:01
  • SRT 1720 dihydrochloride 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].

Name SRT 1720 dihydrochloride
Description SRT 1720 dihydrochloride 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].
Related Catalog
Target

SIRT1:0.10 μM (EC50)

In Vitro 即使在没有 SIRT1 的情况下,SRT 1720 dihydrochloride 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]。
In Vivo SRT 1720 (10, 30, 100 mg/kg, p.o.) dihydrochloride 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 dihydrochloride 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.) dihydrochloride 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]。
Animal Admin Mice: Nine week old C57BL/6 male mice are fed a high fat diet (60% calories from fat) until their mean body weight reach approximately 40 g. The mice are then divided into test groups (6-10 per group). SRT1460 (100 mg/kg), SRT 1720 (100 mg/kg), SRT501 (500 mg/kg) and BRL49653 (5 mg/kg) are administered once daily via oral gavage. The vehicle used is 2% HPMC + 0.2% DOSS. Individual mouse body weights are measured twice weekly. At 2, 4, 6, 8 and 10 weeks of dosing a fed blood glucose measure is taken and after 5 weeks of treatment an IPGTT is conducted on all mice from each of the groups. After 10 weeks of treatment, an ITT is conducted. Statistical analysis is completed using the JMP program. Data are analyzed by a one way ANOVA with comparison to control using a Dunnett’s Test. A p value < 0.05 indicates a significant difference between groups.
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  

[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 emphysema 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 Hypertension by Enhancing AMP-Activated Protein Kinase Activity. Hypertension. 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.  

Molecular Formula C25H25Cl2N7OS
Molecular Weight 542.48