5.05315
A 438079
别名:
A 438079, 3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine hydrochloride, P2X7 Purinergic Receptor Antagonist, A 438079, A438079, A-438079
InChI key
MBTJFFMIPPMRGR-UHFFFAOYSA-N
InChI
1S/C13H9Cl2N5.ClH/c14-11-5-1-4-10(12(11)15)13-17-18-19-20(13)8-9-3-2-6-16-7-9;/h1-7H,8H2;1H
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mM
Quality Level
General description
A potent, competitive, and selective antagonist of P2X7 purinergic receptor (pIC50 = 6.5 nM and 6.9 nM for rat and human P2X7 receptor, respectively). Shown to reduce ATP-induced reactive oxygen species formation in MEL cells by about 87% (~10 µM) and blocks BzATP-stimulated changes in intracellular calcium concentrations (IC50 = 100 and 300 nM at rat and human P2X7 receptors, respectively.
Biochem/physiol Actions
Primary Target
P2X₇
P2X₇
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Donnelly-Roberts, et al., 2007, Br. J. Pharmacol.101, 571.
Wang B, et al., 2013, Purinergic Signal.9, 101.
Wang B, et al., 2013, Purinergic Signal.9, 101.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
D L Donnelly-Roberts et al.
British journal of pharmacology, 151(5), 571-579 (2007-05-02)
ATP-sensitive P2X(7) receptors are localized on cells of immunological origin including peripheral macrophages and glial cells in the CNS. Activation of P2X(7) receptors leads to rapid changes in intracellular calcium concentrations, release of the proinflammatory cytokine interleukin-1beta and following prolonged
Bin Wang et al.
Purinergic signalling, 9(1), 101-112 (2012-09-28)
The presence of P2X7 on erythroid cells is well established, but its physiological role remains unclear. The current study aimed to determine if P2X7 activation induces reactive oxygen species (ROS) formation in murine erythroleukaemia (MEL) cells, a commonly used erythroid
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