| 产品描述： | SRT 1720 is a selective activator of SIRT1 (EC1.5: 0.16 μM) and shows less potent activities on SIRT2/SIRT3 (EC1.5s: 37 μM/300 μM). |
| 靶点： |
Sirtuin |
| 体内研究： |
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/ml/) and rat (bioavailability = 25%, terminal t1/2 = ~8.4 h, AUC = 3,714 ng/h/ml). In DIO mice, fasting blood glucose levels are elevated (120–150 mg dl?1 range) after being placed on a high-fat diet. Administration of SRT1720 reduced fed glucose levels after 1 week of treatment with further reduction after 3 weeks of treatment that continued through 10 weeks of dosing. Glucose excursion during an intraperitoneal glucose tolerance test was also significantly reduced in the SRT1720 group, and comparable to rosiglitazone, a PPARγ activator that has been used to treat type 2 diabetes. SRT1720 attenuated stress-induced premature cellular senescence and protected against emphysema induced by cigarette smoke and elastase in mice. In animal tumour model studies, SRT1720 inhibited MM tumour growth. SRT1720 enhanced the cytotoxic activity of bortezomib or dexamethasone |
| 细胞实验： |
Cell viability was assessed with a colorimetric assay using MTT as described previously. Apoptosis assay was quantified using Annexin V-FITC/Propidium iodide (PI) apoptosis detection kit, as per manufacturer's instructions, followed by analysis on FACS Calibur |
| 动物实验： |
Sirtinol (2 mg/kg) was administered by peritoneal injection, whereas SRT1720 (100 mg/kg) was administered through oral gavage 1 hour prior to CS exposure daily for 3 days. In a separate experiment, SRT1720 (25, 50, and 100 mg/kg) or PHA-408 (50 mg/kg) was dissolved in 0.5% carboxymethylcellulose containing 0.025% Tween 20 and injected via oral gavage into the conscious mice 24 hours prior to elastase administration, which was repeated daily (5 days per week) until 21 days after elastase administration. To study the therapeutic effect on emphysema, SRT1720 (100 mg/kg) was orally administered daily for 2 weeks after the development of elastase-induced emphysema |
| 参考文献： |
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.Su G, Yang W, Wang S, et al. SIRT1-autophagy axis inhibits excess iron-induced ferroptosis of foam cells and subsequently increases IL-1Β and IL-18[J]. Biochemical and Biophysical Research Communications. 2021, 561: 33-39. 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.Wu Q, Hu Y, Jiang M, et al. Effect of Autophagy Regulated by Sirt1/FoxO1 Pathway on the Release of Factors Promoting Thrombosis from Vascular Endothelial Cells[J]. International journal of molecular sciences. 2019, 20(17): 4132. 5.Chauhan D, et al. Preclinical evaluation of a novel SIRT1 modulator SRT1720 in multiple myeloma cells. Br J Haematol. 2011 Dec;155(5):588-98. 6.Chen W, Lin B, Xie S, et al. Naringenin protects RPE cells from NaIO3-induced oxidative damage in vivo and in vitro through up-regulation of SIRT1[J]. Phytomedicine. 2020: 153375. |
| 溶解性： |
DMSO:36 mg/mL (71.1 mM) Ethanol:<1 mg/mL H2O:<1 mg/mL |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.976 ml |
9.881 ml |
19.762 ml |
| 5 mM |
0.395 ml |
1.976 ml |
3.952 ml |
| 10 mM |
0.198 ml |
0.988 ml |
1.976 ml |
| 50 mM |
0.04 ml |
0.198 ml |
0.395 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京