Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PH-797804 是一种 ATP 竞争性的,选择性的p38α/p38β抑制剂,对 p38α 的IC50为 26 nM,Ki 值为 5.8 nM,对 p38β 的Ki 值为 40 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 298 | 现货 | ||
2 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 966 | 现货 | ||
10 mg | ¥ 1,620 | 现货 | ||
25 mg | ¥ 3,390 | 现货 | ||
50 mg | ¥ 4,910 | 现货 | ||
100 mg | ¥ 7,130 | 现货 | ||
200 mg | ¥ 9,590 | 现货 | ||
500 mg | ¥ 14,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 966 | 现货 |
产品描述 | PH-797804 is a pyridinone inhibitor of p38α (IC50: 26 nM, in a cell-free assay); 4-fold more selective versus p38β and does not inhibit JNK2. |
靶点活性 | p38α:26 nM, p38β:102 nM |
体外活性 | PH-797804抗炎活性较强,治疗链球菌细胞壁诱导的关节炎及大小鼠胶原诱导的关节炎时,处理10天可使关节发炎和相关的骨质流失显著降低.在人类Endotoxin 挑战模型中,PH-797804剂量和浓度依赖性地抑制脂多糖诱导的 IL-6,TNF-α和MK-2活性.Endotoxin全身给药大鼠和食蟹猴可造成急性炎症反应,口服PH-797804可有效抑制该反应(ED50:0.07和0.095 mg/kg). |
体内活性 | PH-797804对下述靶点的IC50高于200 μM: CDK2,ERK2,IKK1/2,IKKi,MAPKAP2/3,MKK7 (>100 μM),MNK,MSK (>164 μM),PRAK,RSK2和 TBK1。在人类单核U937细胞系中,PH-797804对脂多糖诱导的TNF-α产生和p38 激酶活性起阻断作用(IC50:5.9/1.1 nM)。作用于U937 细胞时,PH-797804(1 μM)没有抑制JNK 通路(c-Jun 磷酸化)或ERK 通路(ERK 磷酸化)。在原代大鼠骨髓细胞中,PH-797804浓度依赖性地抑制RANKL-和M-CSF诱导的破骨细胞形成(IC50:3 nM)。 |
激酶实验 | P38 kinase assay: A resin capture assay method is used to determine the phosphorylation of epidermal growth factor receptor peptide (EGFRP) or GST-c-Jun by p38 kinases. Reactions mixtures contain 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, ATP (at the indicated concentration), 0.05 to 0.3 μCi of [γ-33P]ATP, 0.8 mM dithiothreitol, and either 200 μM EGFRP or 10 μM GST-c-Jun for p38α kinase reactions. The reaction is initiated by the addition of 25 nM p38α kinase to give a final volume of 50 μl. The p38αkinase reactions are incubated at 25 °C for 30 minutes. Under these conditions, the formation of product for both p38αkinase is linear with time. The reaction is stopped, and the unreacted [γ-33P]ATP is removed by the addition of 150 μl of AG 1 × 8 ion exchange resin in 900 mM sodium formate, pH 3.0. Once thoroughly mixed, solutions are allowed to stand for 5 minutes. A 50-μl aliquot of head volume containing the phosphorylated substrate is removed from the mixture and transferred to a 96-well plate. MicroScint-40 scintillation cocktail (150 μL) is added to each well and the radioactivity quantities using a TopCount NXT microplate scintillation and luminescence counter. |
别名 | PH797804 |
分子量 | 477.3 |
分子式 | C22H19BrF2N2O3 |
CAS No. | 586379-66-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 89 mg/mL (186.5 mM)
Ethanol: 7 mg/mL (14.66 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.0951 mL | 10.4756 mL | 20.9512 mL | 52.378 mL |
5 mM | 0.419 mL | 2.0951 mL | 4.1902 mL | 10.4756 mL | |
10 mM | 0.2095 mL | 1.0476 mL | 2.0951 mL | 5.2378 mL | |
DMSO | 20 mM | 0.1048 mL | 0.5238 mL | 1.0476 mL | 2.6189 mL |
50 mM | 0.0419 mL | 0.2095 mL | 0.419 mL | 1.0476 mL | |
100 mM | 0.021 mL | 0.1048 mL | 0.2095 mL | 0.5238 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。
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