A-438079 hydrochloride

SKU: orb1223717

Description

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

Key Properties

• CAS Number: 899431-18-6
• MW: 342.61
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₀Cl₃N₅
• SMILES: Cl.ClC1=CC=CC(C2=NN=NN2CC2=CN=CC=C2)=C1Cl
• Target: P2 Receptor
• Solubility: Ethanol: 20 mg/mL warmed (58.37 mM); Water: 61 mg/mL (178.04 mM); DMSO: 61 mg/mL (178.04 mM)

Bioactivity

• In Vivo:
  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. 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 has superior neuroprotective effects compared with an equally 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 behaviour scores in the HC model.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

P2 Receptor