A-438079

SKU: orb1305183

Description

A-438079 hydrochloride is a potent and selective P2X7 receptor antagonist (pIC50 = 6.9). It is widely used in vitro and in vivo to investigate the role of P2X7 in neuroinflammation, pain, and immune cell function.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 899431-18-6
• MW: 342.6
• Purity: >98%
• Formula: C₁₃H₉Cl₂N₅·HCl
• SMILES: Cl.Clc1cccc(-c2nnnn2Cc2cccnc2)c1Cl
• Target: Ion channel
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  P2X7:6.9(pIC50)
• In Vivo:
  A-438079 demonstrates selectivity towards the P2X7 receptor at concentrations of up to 100 μM. It effectively inhibits changes in intracellular calcium concentration induced by 10 μM BzATP in 1321N1 cells stably expressing the rat P2X7 receptor, with an IC50 of 321 nM.
• In Vitro:
  A-438079 has the capability to partially, yet significantly, inhibit the depletion of striatal dopamine (DA) levels induced by 6-OHDA. Pretreatment with A-438079 reduces the pain behavior index in the HC model. Intraperitoneal injection of A-438079 (5 and 15 mg/kg) 60 minutes post-epileptic seizure onset diminishes the severity of epileptic episodes and neuronal death within the hippocampus. Additionally, intravenous administration of 80 μMol/kg A-438079 in a neuropathic rat model significantly reduces both noxious and innocuous evoked activities in various categories of spinal neurons.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, A438079, A-438079, A-438079 HCl, A438079 Hydrochloride, A-438079 Hydrochloride, A-438079 hydrochloride, A 438079, A 438079 (hydrochloride), A 438079 hydrochloride, A 438079 Hydrochloride, P2X7, P2XReceptor, P2XRs, P2X Receptor

Compound Identifiers

PubChem CID

11688742