Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SRT 1720 是人 SIRT1 的选择性激活剂 ,EC1.5为 0.16 μM,对 SIRT2 和 SIRT3 的效力要低 230 倍以上。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 490 | 现货 | ||
2 mg | ¥ 733 | 现货 | ||
5 mg | ¥ 1,220 | 现货 | ||
10 mg | ¥ 1,550 | 现货 | ||
25 mg | ¥ 2,990 | 现货 | ||
50 mg | ¥ 4,390 | 现货 | ||
100 mg | ¥ 6,220 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,150 | 现货 |
产品描述 | SRT 1720 is a selective activator of human SIRT1 (EC1.5: 0.16 μM) and is >230-fold less potent for SIRT2 and SIRT3. |
靶点活性 | SIRT1:0.16 μM (EC1.5, cell free), SIRT2:37 μM (EC1.5, cell free) |
体外活性 | The maximum activation ratio of SRT1720 versus the closest sirtuin homologs, SIRT2 (EC1.5 = 37 μM) and SIRT3 (EC1.5 > 300 μM) is up to 781%. SRT1720 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. Higher concentrations of SRT1720 (15 μM) induces a modest (10-20%) decrease in normal cell viability. SRT1720 also significantly inhibits VEGF-dependent MM cell migration [1]. |
体内活性 | SRT 1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinemia 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 the 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]. |
动物实验 | Nine-week-old C57BL/6 male mice are fed a high-fat diet (60% calories from fat) until their mean body weight reaches approximately 40 g. The mice are then divided into test groups (6-10 per group). SRT1460 (100 mg/kg), SRT1720 (100 mg/kg), SRT501 (500 mg/kg) and rosiglitazone (5 mg/kg) are administered once daily via oral gavage. The vehicle used is 2% HPMC + 0.2% DOSS. Individual mouse body weights are measured twice weekly. At 2, 4, 6, 8 and 10 weeks of dosing a fed blood glucose measurement are taken and after 5 weeks of treatment, an IPGTT is conducted on all mice from each of the groups. After 10 weeks of treatment, an ITT is conducted. Statistical analysis is completed using the JMP program. Data are analyzed by a one way ANOVA with a comparison to control using a Dunnett's Test. A p-value < 0.05 indicates a significant difference between groups. |
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 |
分子量 | 469.56 |
分子式 | C25H23N7OS |
CAS No. | 925434-55-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SRT 1720 925434-55-5 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin 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 inhibit Inhibitor SRT1720 SRT-1720 inhibitor