Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and <1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 560 | 35日内发货 | ||
25 mg | ¥ 2,130 | 35日内发货 | ||
100 mg | ¥ 8,640 | 35日内发货 |
产品描述 | AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2]. |
靶点活性 | CK1:, p38β:3.6 nM (ki), JNK3:61 nM (ki), JNK1:11480 nM (ki), JNK2:39 nM (ki), p38α (dog):5.0 nM (ki), p38α:0.5 nM (ki), p38δ:2600 nM (ki), p38γ:4100 nM (ki) |
体外活性 | AMG-548 (10 μM) inhibits the hDvl2 shift[2]. AMG-548 is extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC50=3 nM) and IL1b (IC50=7 nM) as well as TNFa induced IL-8 (IC50=0.7 nM) and IL-1b induced IL-6 (IC5050=1.3 nM) in human whole blood[1]. AMG-548 shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=61 nM). |
体内活性 | The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1]. AMG-548 has rat F of 62% and dog F of 47%. |
分子量 | 461.56 |
分子式 | C29H27N5O |
CAS No. | 864249-60-5 |
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。
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