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SRT 1720 monohydrochloride

MCE China：SRT 1720 monohydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-15145

CAS：2060259-60-9

Purity：98.87%

Storage：4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：SRT 1720 effectively decreases 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：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].

Animal Administration：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

IC50 & Target：SIRT1 0.10 μM (EC50) SIRT1 0.16 μM (EC1.5) SIRT2 37 μM (EC1.5)

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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  [Content Brief]

[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  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[5]. Lahusen TJ, et al. SRT1720 induces lysosomal-dependent cell death of breast cancer cells. Mol Cancer Ther. 2015 Jan;14(1):183-92.  [Content Brief]