Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SRT 2104 (GSK2245840) 是一种高度选择性、可通过血脑屏障的 Sirt1激活剂,依赖于 NAD+,增加 Sirt1 蛋白水平,用于糖尿病和亨廷顿氏症的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 813 | 现货 | ||
10 mg | ¥ 1,310 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,750 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
200 mg | ¥ 7,580 | 现货 | ||
500 mg | ¥ 11,200 | 现货 | ||
1 g | ¥ 14,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 898 | 现货 |
产品描述 | SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator. |
体外活性 | SRT2104 reduces p65/RelA acetylation levels in C2C12 cells.[1] |
体内活性 | In male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard diet, and enhances motor coordination, bone mineral density, and insulin sensitivity and decreased inflammation. Short-term SRT2104 treatment preserves bone and muscle mass in an experimental model of atrophy.[1] In Male N171-82Q HD mice, SRT2104 (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival.[2] |
激酶实验 | SIRT1 fluorescence polarization assay and HTS: In the SIRT1 FP assay, SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2 ) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD +, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2 , 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 ℃ in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths. |
细胞实验 | Cells are cultured in low glucose Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum and penicillin–streptomycin. Cells are treated with vehicle (0.1% DMSO) or 3?μM?SRT2104 for 24?h and then harvested for protein and Western blotting.(Only for Reference) |
别名 | SRT2104, sirtuin modulator, GSK2245840 |
分子量 | 516.64 |
分子式 | C26H24N6O2S2 |
CAS No. | 1093403-33-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 13 mg/mL (25.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9356 mL | 9.6779 mL | 19.3558 mL | 48.3896 mL |
5 mM | 0.3871 mL | 1.9356 mL | 3.8712 mL | 9.6779 mL | |
10 mM | 0.1936 mL | 0.9678 mL | 1.9356 mL | 4.839 mL | |
20 mM | 0.0968 mL | 0.4839 mL | 0.9678 mL | 2.4195 mL |
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 2104 1093403-33-8 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin SRT2104 sirtuin modulator GSK-2245840 GSK2245840 SRT-2104 Inhibitor GSK 2245840 inhibit inhibitor