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Purity: ≥98%
A-438079 HCl (A438079; A 438079), the hydrochloride salt of -438079, is a novel, potent, and selective P2X7 receptor antagonist with anti-Parkinson's disease effects. It inhibits P2X7 receptor with a 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. Blockade of P2X(7) receptors may represent a novel protective strategy for striatal DA terminals in Parkinson's disease.
| ln Vitro |
A 438079, with an IC50 of 321 nM, suppresses BzATP-(10 μM) induced increases in intracellular calcium concentrations in 1321N1 cells that express rat P2X7 receptors consistently. Up to 100 μM of A 438079 is likewise selective for the P2X7 receptor[1].
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| ln Vivo |
In neuropathic rats, 438079 (80 μmol/kg, iv) decreases both benign and harmful evoked activity of various spinal neuron classes. 438079 (i.p., 100 and 300 μmol/kg) as a signi?increases withdrawal thresholds in the SNL and CCI models significantly[1]. A 438079 (5 and 15 mg/kg) injected intraperitoneally 60 minutes after seizures begin lessens the intensity of the convulsions and hippocampal neuronal loss. When A 438079 is administered at the same dose of 25 mg/kg of phenobarbital, the neuroprotective effects are greater[2]. ?A 438079 somewhat, but meaningfully?effectively stops the striatal DA reserves from being depleted by 6-OHDA[3]. In the HC model, pretreatment with A 438079 lowers nociceptive behavior scores[4].
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| References |
[1]. McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28.
[2]. Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64. [3]. Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson's disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7. [4]. Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96 |
| Molecular Formula |
C13H10CL3N5
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| Molecular Weight |
342.61
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| CAS # |
899431-18-6
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| Related CAS # |
899507-36-9
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| SMILES |
ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1.[H]Cl
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9188 mL | 14.5939 mL | 29.1877 mL | |
| 5 mM | 0.5838 mL | 2.9188 mL | 5.8375 mL | |
| 10 mM | 0.2919 mL | 1.4594 mL | 2.9188 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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