Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD7545 是竞争性和选择性的PDHK2抑制剂,能够抑制PDHK1和PDHK2的活性,其IC50值分别为 36.8 nM 和 6.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 659 | 现货 | ||
10 mg | ¥ 1,150 | 现货 | ||
25 mg | ¥ 1,950 | 现货 | ||
50 mg | ¥ 2,880 | 现货 | ||
100 mg | ¥ 4,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 795 | 现货 |
产品描述 | AZD7545 is a potent PDHK inhibitor. |
靶点活性 | PDHK2:6.4 nM, PDHK1:36.8 nM |
体外活性 | 在肥胖的胰岛素抵抗的Zucker大鼠中,AZD7545消除了血糖的餐后升高.AZD7545增加Wistar大鼠中肝脏和骨骼肌中活性PDH的百分比. |
体内活性 | AZD7545通过破坏PDHK2与PDC的二氢硫辛酸乙酰转移酶成分的内部硫辛酰基结构域的相互作用抑制PDHK活性。AZD7545增加原代大鼠肝细胞中PDH活性,EC50为105 nM。在重组人PDHK2存在下,AZD7545增加PDH活性,EC50为5.2 nM。 |
激酶实验 | Cellular Kinase Assays: NIH3T3 cells prepared by transfection of human KDR. The cells are cultured in a collagen type I coated 96-well plate in an amount of 1.5 × 104 per well. The medium is then replaced by a DMEM medium containing 0.1% FCS. Ki8751 diluted in DMSO is added to each well and cultured. rhVEGF is added to a final concentration of 100 ng/mL, and the stimulation of cells is carried out at 37 °C. The cells are washed with PBS (pH 7.4), 50 μL of a solubilization buffer (20 mM HEPES (pH 7.4), 150 mM NaCl, 0.2% Triton X-100, 10% glycerol, 5 mM Na3VO4, 5 mM disodium ethylenediamine tetraacetate, and 2 mM Na4P2O7) is then added and a cell extract is prepared. Separately, PBS (50 μL, pH 7.4) containing 5 μg/mL of antiphosphotyrosine antibody (PY20) is added to a microplate for ELISA. After washing of the plate, 300 μL of a blocking solution is added. The cell extract is transferred to the plate. An anti-VEGFR2 antibody and a peroxidase-labeled anti-rabbit Ig antibody are added. Next, a chromophoric substrate for peroxidase is added, and the absorbance at 450 nm is measured with microplate reader. The VEGFR2 phosphorylation activity for each well is determined by presuming the absorbance with the addition of VEGF and without the addition of the test sample to be 100% VEGFR2 phosphorylation activity and VEGF to be 0% VEGFR2 phosphorylation activity. The concentration of the inhibition (%) of VEGFR2 Phosphorylation is determined for each case, and IC50 value is calculated. |
分子量 | 478.87 |
分子式 | C19H18ClF3N2O5S |
CAS No. | 252017-04-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 88 mg/mL (183.8 mM)
DMSO: 88 mg/mL (183.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.0882 mL | 10.4412 mL | 20.8825 mL | 52.2062 mL |
5 mM | 0.4176 mL | 2.0882 mL | 4.1765 mL | 10.4412 mL | |
10 mM | 0.2088 mL | 1.0441 mL | 2.0882 mL | 5.2206 mL | |
20 mM | 0.1044 mL | 0.5221 mL | 1.0441 mL | 2.6103 mL | |
50 mM | 0.0418 mL | 0.2088 mL | 0.4176 mL | 1.0441 mL | |
100 mM | 0.0209 mL | 0.1044 mL | 0.2088 mL | 0.5221 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。
AZD7545 252017-04-2 Metabolism Dehydrogenase PDH kinase AZD 7545 AZD-7545 inhibit PDHK Pyruvate dehydrogenase kinase Inhibitor inhibitor