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Chemical Structure : Lu AF27139
CAS No.: 2097117-06-9
Catalog No.: PC-38015Not For Human Use, Lab Use Only.
Lu AF27139 is a potent, selective, CNS-penetrant P2X7 receptor antagonist, inhibits BzATP-induced currents in rat primary microglia with IC50 of 66 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $528 | In stock | |
| 100 mg | $1380 | In stock |
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Lu AF27139 is a potent, selective, CNS-penetrant P2X7 receptor antagonist, inhibits BzATP-induced currents in rat primary microglia with IC50 of 66 nM.
Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors.
Lu AF27139 concentration-dependently inhibits IL-1β release in rat ((C50=38 nM) and mouse (IC50=26 nM) primary cortical microglia primed with LPS and induced with 1 mM BzATP.
Lu AF27139 displays favorable PK profile with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability.
Lu AF27139 inhibits LPS- and BzATP-induced IL-1β release in in vivo mouse CNS microdialysis studies.
| M.Wt | 497.921 | |
| Formula | C21H19ClF3N5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-N-(2-(4-chlorophenyl)-2-morpholinoethyl)-2-(pyrimidin-2-yl)-4-(trifluoromethyl)thiazole-5-carboxamide |
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1. Allen T Hopper, et al. J Med Chem. 2021 Apr 22;64(8):4891-4902.
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