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SRT 1720

Catalog No. T5096 CAS 925434-55-5

SRT 1720 is a selective activator of human SIRT1 (EC1.5: 0.16 μM) and is <230-fold less potent for SIRT2 and SIRT3.

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SRT 1720, CAS 925434-55-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 53.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 155.00
50 mg	In stock	$ 272.00
100 mg	In stock	$ 455.00
1 mL * 10 mM (in DMSO)	In stock	$ 92.00

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Purity: 99.7%

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Description	SRT 1720 is a selective activator of human SIRT1 (EC1.5: 0.16 μM) and is >230-fold less potent for SIRT2 and SIRT3.
Targets&IC50	SIRT1:0.16 μM (EC1.5, cell free), SIRT2:37 μM (EC1.5, cell free)
In vitro	The maximum activation ratio of SRT1720 versus the closest sirtuin homologs, SIRT2 (EC1.5 = 37 μM) and SIRT3 (EC1.5 > 300 μM) is up to 781%. SRT1720 binds to the SIRT1 enzyme-peptide substrate complex at an allosteric site amino-terminal to the catalytic domain and lower the Michaelis constant for acetylated substrates. Higher concentrations of SRT1720 (15 μM) induces a modest (10-20%) decrease in normal cell viability. SRT1720 also significantly inhibits VEGF-dependent MM cell migration [1].
In vivo	SRT 1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinemia after 4 weeks, partially normalizing elevated insulin levels similar to rosiglitazone treatment. SRT 1720 treatment significantly reduces fasting blood glucose to near normal levels in Lepob/ob mice[1]. SRT 1720 has the 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 through downstream targets of SIRT1 such as PGC1α and FOXO1[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 Research	Nine-week-old C57BL/6 male mice are fed a high-fat diet (60% calories from fat) until their mean body weight reaches approximately 40 g. The mice are then divided into test groups (6-10 per group). SRT1460 (100 mg/kg), SRT1720 (100 mg/kg), SRT501 (500 mg/kg) and rosiglitazone (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 measurement are 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 a comparison to control using a Dunnett's Test. A p-value < 0.05 indicates a significant difference between groups.

Molecular Weight	469.56
Formula	C25H23N7OS
CAS No.	925434-55-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. Chauhan D, et al. Preclinical evaluation of a novel SIRT1 modulator SRT1720 in multiple myeloma cells. Br J Haematol. 2011 Dec;155(5):588-98. 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. Yu L, et al. Protective effects of SRT1720 via the HNF1α/FXR signalling pathway and anti-inflammatory mechanisms in mice with estrogen-induced cholestatic liver injury. Toxicol Lett. 2016 Dec 15;264:1-11. 5. Wu Q, Hu Y, Jiang M, et al. Effect of Autophagy Regulated by Sirt1/FoxO1 Pathway on the Release of Factors Promoting Thrombosis from Vascular Endothelial Cells[J]. International journal of molecular sciences. 2019, 20(17): 4132.

Citations

1. Wu Q, Hu Y, Jiang M, et al. Effect of Autophagy Regulated by Sirt1/FoxO1 Pathway on the Release of Factors Promoting Thrombosis from Vascular Endothelial Cells. International journal of molecular sciences. 2019, 20(17): 4132. 2. Lian L, Le Z, Wang Z, et al.SIRT1 Inhibits High Glucose–Induced TXNIP/NLRP3 Inflammasome Activation and Cataract Formation.Investigative Ophthalmology & Visual Science.2023, 64(3): 16-16. 3. Li L, Fu S, Wang J, et al.SRT1720 inhibits bladder cancer cell progression by impairing autophagic flux.Biochemical Pharmacology.2024: 116111.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library DNA Damage & Repair Compound Library Anti-Diabetic Compound Library Anti-Metabolism Disease Compound Library Epigenetics Compound Library Histone Modification Compound Library Anti-Aging Compound Library Preclinical Compound Library Bioactive Compound Library Autophagy Compound Library

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Keywords

SRT 1720 925434-55-5 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin inhibit Inhibitor SRT1720 SRT-1720 inhibitor

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