SRT1720 Inhibitor CAS No. 1001645-58-4

Cat. No.	Name	Size	Price
KI0039	SRT1720	5 mg	$300
	SRT1720	10 mg	$560
	SRT1720	50 mg	$1800
	SRT1720	200 mg	$4400

Chemical Characteristic

Product Name	SRT1720
CAS No.	1001645-58-4
Molecular Weight	506.02
Formula	C₂₅H₂₃N₇OS.HCl
Chemical Name	N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide hydrochloride
Smiles	n1c(cnc2ccccc12)C(=O)Nc1c(cccc1)c1nc2scc(n2c1)CN1CCNCC1 Cl
Chemical Structure

Biological activities

SRT1720 is a sirtuin 1 (SIRT1) activator with an EC_{1.5 of 0.16 µM and maximum activation of 781% versus the closest sirtuin homologues, SIRT2 and SIRT3. SRT1720 is efficacy in the treatment of metabolic and chronic diseases associated with aging. 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. ^[1] SRT1720 (3-10 µM) induces mitochondrial biogenesis in renal proximal tubule cells (RPTCs) within 24 hours as determined by elevations in mitochondrial DNA copy number, increases expression of the mitochondrial proteins NADH dehydrogenase 1b subcomplex subunit 8 (NDUFB8) and ATP synthase b, and elevates mitochondrial respiration rates and ATP levels. SRT1720 treatment can also accelerate recovery of mitochondrial functions after acute oxidant injury. SRT1720 increases SIRT1 activity in a concentration-dependent manner with a 3-fold increase in SIRT1 at 1 and 3 µM SRT1720 and a 5-fold increase at 10 µM.^[2] In multiple myeloma (MM) cells, SRT1720 inhibits growth and induces apoptosis resistant to conventional and bortezomib therapies without significantly affecting the viability of normal cells. SRT1720 at 15 µM induces a modest (10-20%) decrease in normal cell viability. ^[3] In short-term in vivo studies, SRT1720 has been demonstrated to enhance insulin sensitivity and improve measures of mitochondrial capacity and oxidative metabolism in obese rats and mice. ^[1] Using a conditional SIRT1 knockout mouse and specific gene knockdowns, SRT1720 affects mitochondrial respiration in a Sirt1- and PGC-1a-dependent manner. SRT1720 also improves body composition, glucose homeostasis and metabolism, suppresses hepatic apoptosis and normalizes gene expression in obese mice. SRT1720 improves insulin sensitivity, maintained liver and pancreatic function, and prevents several metabolic changes associated with a high-fat diet. ^[4] SRT1720 mimics the beneficial effects of calorie restriction on mitochondrial and metabolic function in mammals in vivo and holds promise for treating diseases of ageing such as type 2 diabetes. ^[1]}

References

[1] Milne JC, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007, 450 (7170): 712-716. [2] Funk JA, et al. SRT1720 induces mitochondrial biogenesis and rescues mitochondrial function after oxidant injury in renal proximal tubule cells. J Pharmcol Exp Ther. 2010, 333 (2): 593-601. [3] Chauhan D, et al. Preclinical evaluation of a novel SIRT1 modulator SRT1720 in multiple myeloma cells. Br J Haematol. 2011, 155(5): 588-598. [4] Minor RK, et al. SRT1720 improves survival and healthspan of obese mice. Sci Rep. 2011, 1: 70.

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