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SRT 1720
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SRT 1720图片
CAS NO:925434-55-5
规格:98%
分子量:469.56
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
SRT 1720 是人 SIRT1 的有效激活剂,EC1.5 值为 0.16 μM,同时抑制 SIRT2 和 SIRT3,EC1.5 值分别为 37 μM 和 >300 μM。
CAS:925434-55-5
分子式:C25H23N7OS
分子量:469.56
纯度:98%
存储:Store at -20°C

Background:

SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and >300 μM, respectively. SIRT1|0.16 μM (EC1.5)|SIRT2|37 μM (EC1.5)


SRT 1720 effectively decreases the acetylation of p53 in cells even in the absence of SIRT1, and this is attributed to inhibition of histone acetyltransferase p300[2].


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].


[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 [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 [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. [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.