化合物 T10298L T10298L

Product Introduction
Bioactivity


英文名: AMG-548

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].

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%.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: AMG-548 | AMG 548 | AMG548

相关产品: SB 202190 | VX-702 | Pexmetinib | Atractylenolide II | Rotundic acid | Dehydroglyasperin D | Acumapimod | (±)-Praeruptorin A | Chrysoeriol | PLK1/p38γ-IN-1

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途