A-438079 HCl
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526699

CAS#: 899431-18-6 (HCl); 899507-36-9 (free base)

Description: A-438079 is a P2X7 receptor antagonist. A438079 protects against acetaminophen-induced liver injury by inhibiting p450 isoenzymes, not by inflammasome activation. A-438079 partially but significantly prevented the 6-OHDA-induced depletion of striatal DA stores. P2X7R inhibitor 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.


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A-438079 HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526699
Name: A-438079 HCl
CAS#: 899431-18-6 (HCl); 899507-36-9 (free base)
Chemical Formula: C13H10Cl3N5
Exact Mass:
Molecular Weight: 342.608
Elemental Analysis: C, 45.57; H, 2.94; Cl, 31.04; N, 20.44


Synonym: A-438079 ; A 438079; A438079; A-438079 HCl.

IUPAC/Chemical Name: 3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine hydrochloride

InChi Key: MBTJFFMIPPMRGR-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H9Cl2N5.ClH/c14-11-5-1-4-10(12(11)15)13-17-18-19-20(13)8-9-3-2-6-16-7-9;/h1-7H,8H2;1H

SMILES Code: ClC1=CC=CC(C2=NN=NN2CC3=CN=CC=C3)=C1Cl.Cl


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

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2: Nieto FR, Clark AK, Grist J, Hathway GJ, Chapman V, Malcangio M. Neuron-immune mechanisms contribute to pain in early stages of arthritis. J Neuroinflammation. 2016 Apr 29;13(1):96. doi: 10.1186/s12974-016-0556-0. PubMed PMID: 27130316; PubMed Central PMCID: PMC4851814.

3: Fernandes NC, Sriram U, Gofman L, Cenna JM, Ramirez SH, Potula R. Methamphetamine alters microglial immune function through P2X7R signaling. J Neuroinflammation. 2016 Apr 26;13(1):91. doi: 10.1186/s12974-016-0553-3. PubMed PMID: 27117066; PubMed Central PMCID: PMC4847215.

4: Barros-Barbosa AR, Fonseca AL, Guerra-Gomes S, Ferreirinha F, Santos A, Rangel R, Lobo MG, Correia-de-Sá P, Cordeiro JM. Up-regulation of P2X7 receptor-mediated inhibition of GABA uptake by nerve terminals of the human epileptic neocortex. Epilepsia. 2016 Jan;57(1):99-110. doi: 10.1111/epi.13263. Epub 2015 Dec 30. PubMed PMID: 26714441.

5: Xu J, Chen XM, Zheng BJ, Wang XR. Electroacupuncture Relieves Nerve Injury-Induced Pain Hypersensitivity via the Inhibition of Spinal P2X7 Receptor-Positive Microglia. Anesth Analg. 2016 Mar;122(3):882-92. doi: 10.1213/ANE.0000000000001097. PubMed PMID: 26599792.

6: Barros-Barbosa AR, Lobo MG, Ferreirinha F, Correia-de-Sá P, Cordeiro JM. P2X7 receptor activation downmodulates Na(+)-dependent high-affinity GABA and glutamate transport into rat brain cortex synaptosomes. Neuroscience. 2015 Oct 15;306:74-90. doi: 10.1016/j.neuroscience.2015.08.026. Epub 2015 Aug 20. PubMed PMID: 26299340.

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10: Yan Y, Bai J, Zhou X, Tang J, Jiang C, Tolbert E, Bayliss G, Gong R, Zhao TC, Zhuang S. P2X7 receptor inhibition protects against ischemic acute kidney injury in mice. Am J Physiol Cell Physiol. 2015 Mar 15;308(6):C463-72. doi: 10.1152/ajpcell.00245.2014. Epub 2015 Jan 14. PubMed PMID: 25588875; PubMed Central PMCID: PMC4360025.

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12: Zhang Y, Yuan F, Cao X, Zhai Z, GangHuang, Du X, Wang Y, Zhang J, Huang Y, Zhao J, Hou W. P2X7 receptor blockade protects against cisplatin-induced nephrotoxicity in mice by decreasing the activities of inflammasome components, oxidative stress and caspase-3. Toxicol Appl Pharmacol. 2014 Oct 12;281(1):1-10. doi: 10.1016/j.taap.2014.09.016. [Epub ahead of print] PubMed PMID: 25308879.

13: Ying YL, Wei XH, Xu XB, She SZ, Zhou LJ, Lv J, Li D, Zheng B, Liu XG. Over-expression of P2X7 receptors in spinal glial cells contributes to the development of chronic postsurgical pain induced by skin/muscle incision and retraction (SMIR) in rats. Exp Neurol. 2014 Nov;261:836-43. doi: 10.1016/j.expneurol.2014.09.007. Epub 2014 Sep 19. PubMed PMID: 25242211.

14: Teixeira JM, de Oliveira-Fusaro MC, Parada CA, Tambeli CH. Peripheral P2X7 receptor-induced mechanical hyperalgesia is mediated by bradykinin. Neuroscience. 2014 Sep 26;277:163-73. doi: 10.1016/j.neuroscience.2014.06.057. Epub 2014 Jul 2. PubMed PMID: 24997266.

15: Ficker C, Rozmer K, Kató E, Andó RD, Schumann L, Krügel U, Franke H, Sperlágh B, Riedel T, Illes P. Astrocyte-neuron interaction in the substantia gelatinosa of the spinal cord dorsal horn via P2X7 receptor-mediated release of glutamate and reactive oxygen species. Glia. 2014 Oct;62(10):1671-86. doi: 10.1002/glia.22707. Epub 2014 Jun 4. PubMed PMID: 24895290.

16: Mesuret G, Engel T, Hessel EV, Sanz-Rodriguez A, Jimenez-Pacheco A, Miras-Portugal MT, Diaz-Hernandez M, Henshall DC. P2X7 receptor inhibition interrupts the progression of seizures in immature rats and reduces hippocampal damage. CNS Neurosci Ther. 2014 Jun;20(6):556-64. doi: 10.1111/cns.12272. Epub 2014 Apr 21. PubMed PMID: 24750893.

17: Rubio-Araiz A, Perez-Hernandez M, Urrutia A, Porcu F, Borcel E, Gutierrez-Lopez MD, O'Shea E, Colado MI. 3,4-Methylenedioxymethamphetamine (MDMA, ecstasy) disrupts blood-brain barrier integrity through a mechanism involving P2X7 receptors. Int J Neuropsychopharmacol. 2014 Aug;17(8):1243-55. doi: 10.1017/S1461145714000145. Epub 2014 Mar 14. PubMed PMID: 24626059.

18: Bełtowski J, Guranowski A, Jamroz-Wiśniewska A, Korolczuk A, Wojtak A. Nucleoside monophosphorothioates as the new hydrogen sulfide precursors with unique properties. Pharmacol Res. 2014 Mar;81:34-43. doi: 10.1016/j.phrs.2014.01.003. Epub 2014 Feb 5. PubMed PMID: 24508566.

19: Schoenauer R, Atanassoff AP, Wolfmeier H, Pelegrin P, Babiychuk EB, Draeger A. P2X7 receptors mediate resistance to toxin-induced cell lysis. Biochim Biophys Acta. 2014 May;1843(5):915-22. doi: 10.1016/j.bbamcr.2014.01.024. Epub 2014 Jan 31. PubMed PMID: 24487066.

20: Gicquel T, Victoni T, Fautrel A, Robert S, Gleonnec F, Guezingar M, Couillin I, Catros V, Boichot E, Lagente V. Involvement of purinergic receptors and NOD-like receptor-family protein 3-inflammasome pathway in the adenosine triphosphate-induced cytokine release from macrophages. Clin Exp Pharmacol Physiol. 2014 Apr;41(4):279-86. doi: 10.1111/1440-1681.12214. PubMed PMID: 24472059.