| Identification | Back Directory | [Name]
N-[2-[3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide | [CAS]
925434-55-5 | [Synonyms]
SRT1720 free base/ STR1720 HCl salt
SRT1720 - CAS 925434-55-5 - Calbiochem
N-[2-[3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide
N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide
2-QuinoxalinecarboxaMide, N-[2-[3-(1-piperazinylMethyl)iMidazo[2,1-b]thiazol-6-yl]phenyl]-
N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide
Quinoxaline-2-carboxylic acid [2-(3-piperazin-1-ylmethyl-imidazo[2,1-b]thiazol-6-yl)-phenyl]-amide | [Molecular Formula]
C25H23N7OS | [MDL Number]
MFCD14584468 | [MOL File]
925434-55-5.mol | [Molecular Weight]
469.56 |
| Chemical Properties | Back Directory | [Melting point ]
221℃ | [density ]
1.46 | [storage temp. ]
-20C | [solubility ]
DMSO:5.0(Max Conc. mg/mL);10.65(Max Conc. mM) | [form ]
Yellow solid | [pka]
11.19±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively. | [General Description]
A cell-permeable quinolinecarboxamide compound that is shown to inhibit the mitochondrial SIRT3 in a substrate AceCS2-competitive (Ki = 0.56 μM; Km = 2.44 μM), but NAD+-uncompetitive (Ki = 0.34 μM; Km = 280 μM), manner. Also reported to decrease cellular p53 Lys382 acetylation (Effective conc. = 10 μM in U2OS and MEF cultures) and inhibit p300 HAT activity (IC50 = 9 μM) in vitro, as well as offer therapeutic benefits in several murine and rodent type 2 diabetes models (100 mg/kg/dayl p.o.) in vivo. Whether and how SRT1720 activates SIRT1 activity remains uncertain. Also available as a 25 mM solution in DMSO (Cat. No. 530748). | [in vivo]
SRT 1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinaemia 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 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]. | [IC 50]
SIRT1: 0.16 μM (EC1.5); SIRT2: 37 μM (EC1.5) | [storage]
Store at -20°C | [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] 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. DOI:10.1016/j.toxlet.2016.10.016 |
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