An antagonist of the nucleotide receptor P2X7
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A-438079 (hydrochloride)

Item No. 14580

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl]methyl]-pyridine, monohydrochloride
CAS Number
899431-18-6
Molecular Formula
C13H9Cl2N5 • HCl
Formula Weight
342.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.33 mg/mlEthanol: 10 mg/ml
SMILES
ClC1=C(Cl)C=CC=C1C2=NN=NN2CC3=CN=CC=C3.Cl
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
InChi Key
MBTJFFMIPPMRGR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $98

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    10 mg

    $185

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    25 mg

    $363

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    50 mg

    $627

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    Product Description

    A-438079 is a competitive antagonist of the nucleotide receptor P2X7 (pIC50 = 6.9).1 It inhibits both calcium flux and IL-1β release mediated by P2X7 while not affecting the activity of other P2X receptors.1,2 A-438079 is effective in evaluating the role of P2X7 in nociception, oxidative stress, and apoptosis in cells and animals.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nelson, D.W., Gregg, R.J., Kort, M.E., et al. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. J. Med. Chem. 49(12), 3659-3666 (2006).

    2. Donnelly-Roberts, D.L., and Jarvis, M.F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. Br. J. Pharmacol. 151(5), 571-579 (2007).

    3. McGaraughty, S., Chu, K.L., Namovic, M.T., et al. P2X7-related modulation of pathological nociception in rats. Neuroscience 146(4), 1817-1828 (2007).

    4. Haanes, K.A., Schwab, A., and Novak, I. The P2X7 receptor supports both life and death in fibrogenic pancreatic stellate cells. PLoS One 7(12), (2012).

    5. Bartlett, R., Yerbury, J.J., and Sluyter, R. P2X7 receptor activation induces reactive oxygen species formation and cell death in murine EOC13 microglia. Mediators Inflamm. 271813, (2013).