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A 438079

SKU: orb1940834

Description

A 438079 is a potent, and selective antagonist of P2X7 receptor (pIC50: 6.9).(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.(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.

Images & Validation

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A 438079

Key Properties

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CAS Number899507-36-9
MW306.15
Purity>98% (HPLC)
FormulaC13H9Cl2N5
SMILESClc1cccc(-c2nnnn2Cc2cccnc2)c1Cl
TargetP2X Receptor
SolubilityIn Vitro: DMSO : 100 mg/mL (326.64 mM)

Bioactivity

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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

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Quick Database Links

Gene Symbol
P2X Receptor

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