| 名称 | Lu AF27139 |
| 描述 | Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies. |
| 体外活性 | Lu AF27139 (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose. Lu AF27139 inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC50 of 38 ± 2.5 nM. Lu AF27139 concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice. Lu AF27139 (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC50 of 66 nM[1]. |
| 体内活性 | In male Sprague−Dawley rats and male C57BL mice, Lu AF27139 (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 溶解度 | DMSO : 120 mg/mL (241.00 mM) |
| 关键字 | Inhibitor | P2XRs | Lu AF-27139 | oral | P2X7 | Lu AF 27139 | rodent-active | CNS-penetrant | Lu AF27139 | CNS | inhibit | P2X Receptor |
| 相关产品 | A 438079 hydrochloride | BX430 | Brilliant blue G-250 | Gefapixant | Opiranserin hydrochloride | Camlipixant | GSK-1482160 | A-740003 | (E/Z)-Sivopixant | PPADS tetrasodium |
| 相关库 | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | Bioactive Compound Library |
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