Home Neuronal Signaling P2 Receptor antagonist A-438079 HCl For research use only.

A-438079 HCl

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

A-438079 HCl Chemical Structure

A-438079 HCl Chemical Structure

CAS No. 899431-18-6

Purity & Quality Control

A-438079 HCl Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Function assay Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay, IC50=0.12303 μM 21536435
human 1321N1 cells Function assay Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR, IC50=0.12589 μM 16759108
human THP1 cells Function assay Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake, IC50=0.12589 μM 19191585
HEK cells Function assay Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake, IC50=0.31623 μM 19191585
Click to View More Cell Line Experimental Data

Biological Activity

Description A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
Targets
P2X7 [1]
(in 1321N1 cells)
6.9(pIC50)
In vitro
In vitro

In 1321N1 cells stably expressing rat P2X7 receptors, A-438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM. A-438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM.[1]
In Vivo
In vivo

Intraperitoneal injection of A-438079 (5 and 15 mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus.A-438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores.[3] Pretreatment with A-438079 reduces nociceptive behaviour scores in the HC model.[4] A-438079 (80 μmol/kg, i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats. A-438079 (100 and 300 μmol/kg, i.p.) significantly raises withdrawal thresh-olds in both the SNL and CCI models.[1]
Animal Research Animal Models Sprague-Dawley male rats
Dosages 30 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 342.61 Formula

C13H10Cl3N5
CAS No. 899431-18-6 SDF Download A-438079 HCl SDF
Smiles C1=CC(=C(C(=C1)Cl)Cl)C2=NN=NN2CC3=CN=CC=C3.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (198.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 68 mg/mL

Ethanol : 68 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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