化合物A804598 T3639
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Product IntroductionBioactivity英文名: A-804598描述: A-804598 是一个 CNS 渗透，竞争性和选择性的 P2X7受体拮抗剂，作用于小鼠、大鼠和人的 P2X7 受体，IC50s 分别是 9、10
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Product Introduction
Bioactivity
英文名: A-804598
描述: A-804598 是一个 CNS 渗透，竞争性和选择性的 P2X7受体拮抗剂，作用于小鼠、大鼠和人的 P2X7 受体，IC50s 分别是 9、10 和 11 nM。
体外活性: A-804598 effectively blocked IL-1β release in the THP-1 cells (IC50: 8.5 nM). It also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50: 8.1 nM) with similar potency as in the calcium-influx assay. [1]
体内活性: According to the autoradiographic analysis of coronal rat brain sections, there was specific binding of [3H]-A-804598 throughout the rat brain. In the grey matter of the L4-L6 region of the rat spinal cord, it was also found that high levels of [3H]-A-804598 specific binding. [2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 31.5 mg/mL(100 mM)
关键字: A-804598 | P2X Receptor | A804598 | P2XRs | Inhibitor | inhibit
相关产品: BX430 | Brilliant blue G-250 | Gefapixant | GW791343 dihydrochloride | KN-62 | Oxatomide | BzATP triethylammonium salt | A-317491 | Lu AF27139 | RO-3
相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
Bioactivity
英文名: A-804598
描述: A-804598 是一个 CNS 渗透，竞争性和选择性的 P2X7受体拮抗剂，作用于小鼠、大鼠和人的 P2X7 受体，IC50s 分别是 9、10 和 11 nM。
体外活性: A-804598 effectively blocked IL-1β release in the THP-1 cells (IC50: 8.5 nM). It also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50: 8.1 nM) with similar potency as in the calcium-influx assay. [1]
体内活性: According to the autoradiographic analysis of coronal rat brain sections, there was specific binding of [3H]-A-804598 throughout the rat brain. In the grey matter of the L4-L6 region of the rat spinal cord, it was also found that high levels of [3H]-A-804598 specific binding. [2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 31.5 mg/mL(100 mM)
关键字: A-804598 | P2X Receptor | A804598 | P2XRs | Inhibitor | inhibit
相关产品: BX430 | Brilliant blue G-250 | Gefapixant | GW791343 dihydrochloride | KN-62 | Oxatomide | BzATP triethylammonium salt | A-317491 | Lu AF27139 | RO-3
相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
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