A 438079

SKU: orb1310032

Description

A 438079 is a potent and selective P2X7 receptor antagonist with a pIC50 of 6.9. This small molecule is a valuable research tool for investigating the role of P2X7 in inflammatory and neurological processes, supporting both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 899507-36-9
• MW: 306.15
• Purity: 99.82% (May vary between batches)
• Formula: C₁₃H₉Cl₂N₅
• SMILES: Clc1cccc(-c2nnnn2Cc2cccnc2)c1Cl
• Target: P2X Receptor
• Solubility: DMSO:145 mg/mL (473.62 mM);H2O:0.2 mg/mL (0.65 mM)

Bioactivity

• Target IC50:
  P2X7 receptor:6.9(pIC50)
• In Vivo:
  In neuropathic rats noxious and innocuous evoked activity of different classes of spinal neurons is reduced by A 438079 (80 μmol/kg, i.v.), and it significantly raises withdrawal thresh-olds in both the SNL and CCI models. A 438079 has superior neuroprotective effects compared with an equal dose of phenobarbital (25 mg/kg). A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A 438079 reduces nociceptive behavior scores in the HC model.
• In Vitro:
  A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM in 1321N1 cells stably expressing rat P2X7 receptors. A 438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM.
• Animal Research:
  To confirm A 438079 reach the brain after systemic administration, P10 rat pups are injected with 5 mg/kg A 438079 and killed either 10 min, 30 min, or 2 h later (n=4 per group). Blood samples are centrifuged at 1000×g for 10 min to isolate the plasma. Samples are analyzed using LC-MS/MS by a service provider. Briefly, protein is precipitated from 50 μL aliquots of the individual plasma or brain tissue homogenate, and A 438079 is quantified by LC-MS/MS from a five-point standard curve .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, A 438079, A438079, A-438079, P2X7 receptor, P2X7, P2XReceptor, P2XRs, P2X Receptor

Compound Identifiers

PubChem CID

11673921