CAS NO: | 925434-55-5 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 询价 |
10mg | 询价 |
50mg | 询价 |
Cas No. | 925434-55-5 |
别名 | N-[2-[3-(1-哌嗪基甲基)咪唑并[2,1-B]噻唑-6-基]苯基]-2-喹喔啉甲酰胺 |
Canonical SMILES | O=C(NC1=C(C=CC=C1)C2=CN3C(SC=C3CN4CCNCC4)=N2)C5=NC6=C(N=C5)C=CC=C6 |
分子式 | C25H23N7OS |
分子量 | 469.56 |
溶解度 | DMSO : 62.5 mg/mL (133.10 mM; ultrasonic and adjust pH to 5 with HCl) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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. |
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