product name A-438079 HCl
Description: A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. A438079 protects against acetaminophen-induced liver injury by inhibiting p450 isoenzymes, not by inflammasome activation. A-438079 reduced electrographic and clinical seizure severity during status epilepticus and reduced seizure-induced neuronal death in the neocortex.
References: Neuroscience. 2007 Jun 8;146(4):1817-28; CNS Neurosci Ther. 2014 Jun;20(6):556-64.
342.61
Formula
C13H10Cl3N5
CAS No.
899431-18-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 61 mg/mL (178.0 mM)
Water: 61 mg/mL (178.0 mM)
Ethanol: 20 mg/mL warmed (58.4 mM)
Solubility (In vivo)
Saline: 30mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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 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. 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. |
| Animal model | Sprague-Dawley male rats |
| Formulation & Dosage | Dissolved in Saline; 30 mg/kg; i.p. |
| References | Neuroscience. 2007 Jun 8;146(4):1817-28; CNS Neurosci Ther. 2014 Jun;20(6):556-64. |
