Chemical Structure : AZ11645373
货号: PC-22910Not For Human Use, Lab Use Only.
AZ11645373 is a selective and potent antagonist of human P2X7 receptor, inhibits ATP-mediated release of IL-1β in LPS-stimulated THP-1 monocytes with Kb of 92 nM.
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AZ11645373 is a selective and potent antagonist of human P2X7 receptor, inhibits ATP-mediated release of IL-1β in LPS-stimulated THP-1 monocytes with Kb of 92 nM.
AZ11645373 has no agonist or antagonist actions on membrane currents due to P2X receptor activation at human P2X(1), rat P2X(2), human P2X(3), rat P2X(2/3), human P2X(4), or human P2X(5) receptors expressed in HEK cells.
AZ11645373 inhibits ATP- or BzATP-evoked YO-PRO1 fluorescence in HEK cells stably expressing hP2X7R, but not rP2X7R-expressing cells.
AZ11645373 is highly effective at inhibiting ATP- and BzATP-mediated responses in all our assays on hP2X7Rs, with IC50/KB values ranging from 5 to 90 nM depending on the specific assay.
分子量 | 463.51 | |
分子式 | C24H21N3O5S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Laurent C, et al. Br J Pharmacol. 2006 Dec;149(7):880-7.
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