Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMX-5804 是一种口服有活性的MAP4K4选择性抑制剂,其对人 MAP4K4 的IC50=3 nM,pIC50=8.55。对 MINK1/MAP4K6 (pIC50=8.18) 和 TNIK/MAP4K7 (pIC50=7.96) 的作用相对较弱。它可以提高心肌细胞存活率,降低小鼠的缺血再灌注损伤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 948 | 现货 | ||
2 mg | ¥ 1,420 | 现货 | ||
5 mg | ¥ 2,390 | 现货 | ||
10 mg | ¥ 3,850 | 现货 | ||
25 mg | ¥ 6,190 | 现货 | ||
50 mg | ¥ 8,520 | 现货 | ||
100 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,630 | 现货 |
产品描述 | DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice. |
靶点活性 | MAP4K4:3 nM |
体外活性 | DMX-5804, that rescues cell survival, mitochondrial function. |
体内活性 | DMX-5804 reduces ischemia-reperfusion injury in mice by more than 50%. |
细胞实验 | Mitochondrial function in hiPSC-CMs was determined using a Seahorse XFe24 Analyzer.?vCor.4U cells (60,000/well) were transferred to 0.1% gelatin-coated XF24 plates and maintained for 5 d. On day 6, DMX-5804 was added 45 min prior to challenge with menadione for 2 h. The medium was replaced 1 hr before the assay, using bicarbonate-free Seahorse assay medium (8.3 g L-1 DMEM Base , 10 mM glucose, 2 mM L-alanyl-L-glutamine dipeptide, 1 mM sodium pyruvate , pH 7.4).?Cells were maintained at 37 C without supplemental CO2 starting 1 hr before the assay.?For each state measured, three assay cycles were performed (4 min mixing, 2 min wait, and 2 min measurement periods, with readings every 15 s). The basal oxygen consumption rate (OCR) and extracellular acidification rate were determined, followed by sequential injection of 1 μM oligomycin A to inhibit ATP synthase, 0.5 μM carbonyl cyanide-4-phenylhydrazone to uncouple oxidative phosphorylation, and 1 μM antimycin A/rotenone to inhibit mitochondrial complex III and I. For each condition, 12 wells were tested, comprising 4 independent experiments. |
动物实验 | n vivo pharmacokinetic profiling was performed in female CD-1 mice, using 3 animals per time point.?First, 30% w/v Kleptose as excipient was dissolved in water and vortexed gently for several min. Next, 30 mg of DMX-5084?was dissolved into 0.6 mL of DMSO, for a concentration of 50 mg ml-1, and 4.5 mL of the Kleptose solution was added to 0.5 mL of the test compound solution.?A precipitate forms, which re-dissolves over 2-5 min, leaving a clear or slightly hazy solution with a final concentration of 5 mg/ml.?The dosing solution is used as soon as practicable, vortexing immediately prior to use.?This amount was sufficient formulation for 25 doses of 200 μL (20 g mouse).?Compounds were administered orally at 50 mg/kg, with terminal blood (plasma) sampling at 10 min, 30 min, 1 h, 2.5 h, 5 h, 10 h, and 20 h[1]. |
别名 | DMX-5084 |
分子量 | 361.39 |
分子式 | C21H19N3O3 |
CAS No. | 2306178-56-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (345.89 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7671 mL | 13.8355 mL | 27.6709 mL | 69.1773 mL |
5 mM | 0.5534 mL | 2.7671 mL | 5.5342 mL | 13.8355 mL | |
10 mM | 0.2767 mL | 1.3835 mL | 2.7671 mL | 6.9177 mL | |
20 mM | 0.1384 mL | 0.6918 mL | 1.3835 mL | 3.4589 mL | |
50 mM | 0.0553 mL | 0.2767 mL | 0.5534 mL | 1.3835 mL | |
100 mM | 0.0277 mL | 0.1384 mL | 0.2767 mL | 0.6918 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。
DMX-5804 2306178-56-1 MAPK inhibit Inhibitor MAP4K DMX5084 DMX-5084 DMX5804 DMX 5084 DMX 5804 MAPK Kinase Kinase Kinase inhibitor