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A438079 Inhibitor – A 438079

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752648

MBS5752648 is an inhibitor targeting A438079. Also known as A 438079. A 438079 is a potent, and selective antagonist of P2X7 receptor (pIC50: 6.9). More details

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Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
A 438079 (A438079), Inhibitor
Full Product Name
A 438079
Product Gene Name
A438079, inhibitor
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
306.15
Solubility
H2O: 0.2mg/mL (0.65mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C13H9Cl2N5
SMILES
ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1
CAS Number
899507-36-9
Target & IC50
P2X7 receptor: ic50 6.9 (pIC50)
Kinase Assay
Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1 and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+ concentrations are assessed in all of the cell lines using the Ca2+ chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 minutes. Ligands are tested at 11 half-log concentrations from 0.1nM to 100uM. BzATP or ATP concentrations corresponds to the EC70 values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and fluorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 minutes. The pEC50 or pIC50 values are derived from a single curve fit [1].

Product Categories/Family for A438079, inhibitor

Neuroscience; P2 Receptor

Product References and Citations for A438079, inhibitor

McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28.
McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28.
Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64.
Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64.
Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7.
Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7.
Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96.
Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96.

Other Notes

Small volumes of A438079, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.
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