1001645-58-4

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SRT1720/SRT-1720

1001645-58-4

编号ABP000371 化学名称SRT1720/SRT-1720 英文名称 SRT1720/SRT-1720 MDL: MFCD18074509 分子式C25H23N7OS.ClH 分子量506.032 纯度 >98%

化学名称 : SRT1720/SRT-1720

CAS : 1001645-58-4

英文名称: SRT1720/SRT-1720

英文同义词: N-[2-[3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide hydrochloride;SRT1720

溶解度:DMSO

储存条件:at -20C 2 years

生物活性

SRT1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 µM and maximum activation = 781%) versus the closest sirtuin homologues, SIRT2 and SIRT3,(SIRT2: EC1.5 = 37 µM��SIRT3: EC1.5 > 300 µM). This agent 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.SRT1720 exhibited a pharmacokinetic profile suitable for in vivo evaluation in both mouse (bioavailability = 50%, terminal t1/2 = ~5 h, Area Under the Curve (AUC) = 7,892 ng h−1 ml−1) and rat (bioavailability = 25%, terminal t1/2 = ~8.4 h, AUC = 3,714 ng h−1 ml−1).In diet-induced obese and genetically obese mice, SRT1720 improved insulin sensitivity, lower plasma glucose, and increase mitochondrial capacity. Thus, SRT1720 is a promising new therapeutic agent for treating diseases of ageing such as type 2 diabetes.

参考文献

1. Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, Jin L, Boss O, Perni RB, Vu CB, Bemis JE, Xie R, Disch JS, Ng PY, Nunes JJ, Lynch AV, Yang H, Galonek H, Israelian K, Choy W, Iffland A, Lavu S, Medvedik O, Sinclair DA, Olefsky JM, Jirousek MR, Elliott PJ, Westphal CH. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29;450(7170):712-6. 2. Feige JN, Lagouge M, Canto C, Strehle A, Houten SM, Milne JC, Lambert PD, Mataki C, Elliott PJ, Auwerx J. Specific SIRT1 activation mimics low energy levels and protects against diet-induced metabolic disorders by enhancing fat oxidation. Cell Metab. 2008 Nov;8(5):347-58. Erratum in: Cell Metab. 2009 Feb;9(2):210. 3. Yamazaki Y, Usui I, Kanatani Y, Matsuya Y, Tsuneyama K, Fujisaka S, Bukhari A, Suzuki H, Senda S, Imanishi S, Hirata K, Ishiki M, Hayashi R, Urakaze M, Nemoto H, Kobayashi M, Tobe K. Treatment with SRT1720, a SIRT1 Activator, Ameliorates Fatty Liver with Reduced Expression of Lipogenic Enzymes in MSG Mice. Am J Physiol Endocrinol Metab. 2009 Sep 1

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