化合物HA130 T2646

Product Introduction
Bioactivity


英文名: HA130

描述: HA130 是选择性 autotaxin 抑制剂，IC50=28 nM。

激酶实验: Saturation, association, and dissociation binding studies are performed for [3H]Vilanterol to determine receptor binding kinetics at the β2-AR (equilibrium dissociation constant (KD), total number of receptors (Bmax), association rate (kon), and dissociation rate (koff) are calculated). For saturation binding, membranes (in a volume of 1.4 mL to avoid ligand depletion) are incubated with increasing concentrations of [3H]Vilanterol (~0.01-1.3 nM) for 5 h before filtration. For association binding, membranes are incubated with different concentrations of [3H]Vilanterol (~0.1-1.9 nM) for varying incubation times up to 1 h before filtration. For dissociation binding, membranes are preincubated for 1 h with a fixed concentration of [3H]Vilanterol (~1.1 nM) before dissociation is initiated by a 1:20 dilution in binding buffer (containing 10 μM cold Vilanterol) and then incubated for varying times up to 8 h before filtration. Saturation binding is also completed for [3H]CGP12177 (increasing concentrations of ~0.01-2.8 nM) in the same format as described above for [3H]Vilanterol. To determine the affinity of β2-AR agonists and antagonists, competition binding displacement studies are completed in which membranes are incubated with a fixed concentration of [3H]Vilanterol (~0.2 nM) and increasing concentrations of unlabeled agonist/antagonist for 5 h before filtration. All competition binding displacement studies are completed in the presence of 100 μM Gpp(NH)p to ensure that binding curves are monophasic[1].

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

溶解度: DMSO : 46.33 mg/mL (100 mM)


关键字: inhibit | HA-130 | HA 130 | Phosphodiesterase (PDE) | Inhibitor | HA130

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相关库: Anti-Neurodegenerative Disease Compound Library | Bioactive Lipid Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Anti-Alzheimer's Disease Compound Library | Anti-Cardiovascular Disease Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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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