ChemicalBook CAS DataBase List 2468639-77-0

2468639-77-0

Name	2-Quinoxalinecarboxamide, N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-, hydrochloride (1:2)
CAS	2468639-77-0
Molecular Formula	C25H24ClN7OS
Molecular Weight	506.03
MOL File	2468639-77-0.mol

Chemical Properties

form	Solid
color	Brown to orange

Hazard Information

Uses

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].

in vivo

SRT 1720 (10, 30, 100 mg/kg, p.o.) dihydrochloride treatment significantly reduces fasting blood glucose to near normal levels in Lep^ob/ob mice^[1]. SRT 1720 dihydrochloride 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 through downstream targets of SIRT1 such as PGC1α and FOXO1^[2]. SRT 1720 (50-100 mg/kg, p.o.) dihydrochloride, during emphysema development attenuates elastase-induced airspace enlargement and lung function impairment as well as reduces arterial oxygen saturation in WT mice^[3].

IC 50

SIRT1: 0.10 μM (EC₅₀)

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 DOI:10.1038/nature06261
[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 DOI:10.1038/nrd3738
[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. DOI:10.1172/JCI60132
[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. DOI:10.1161/HYPERTENSIONAHA.116.07709
[5] Lahusen TJ, et al. SRT1720 induces lysosomal-dependent cell death of breast cancer cells. Mol Cancer Ther. 2015 Jan;14(1):183-92. DOI:10.1158/1535-7163.MCT-14-0584

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