现货,SRT1720,CAS号:1001645-58-4,美国进口,HDAC-HSP-Aurora,Sirtuin ,Sirtuin 抑制剂和化合物,S1129,selleck ,

信号转导通路: HDAC-HSP-Aurora >> Sirtuin >> Sirtuin 抑制剂 >> SRT1720http://selleck.cn/srt1720-S1129.html

技术数据:

分子量(MW): 506.02

化学式:

C25H23N7OS.HCl

 

溶解度: DMSO ≥101mg/mL Water ≥23mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1001645-58-4

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. [1]

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). [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.[1]

However, the claim that SRT-1720 is a SIRT1 activator has been questioned. [2,3]

 

 

 

参考文献

Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes Milne JC, et al. Nature. 2007 Nov 29;450(7170):712-6.

SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1 Pacholec M, Chrunyk BA,et al. J Biol Chem. 2010 Mar 12;285(11):8340-51.

Beher D, Wu J,et al. Drug Des. 2009;74, 619–624

 

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