A P2X7 receptor antagonist
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A-839977

Item No. 30934

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(2,3-dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine
CAS Number
870061-27-1
Molecular Formula
C19H14Cl2N6O
Formula Weight
413.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
ClC1=CC=CC(N2C(NCC3=CC=CC=C3OC4=CC=CC=N4)=NN=N2)=C1Cl
InChi Code
InChI=1S/C19H14Cl2N6O/c20-14-7-5-8-15(18(14)21)27-19(24-25-26-27)23-12-13-6-1-2-9-16(13)28-17-10-3-4-11-22-17/h1-11H,12H2,(H,23,24,26)
InChi Key
GMVNBKZQJFRFAR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    10 mg

    $236

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    Cayman Chemical
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    Product Description

    A-389977 is an antagonist of the purinergic P2X7 receptor.1 It inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human, rat, and mouse receptors (IC50s = 20, 42, and 150 nM, respectively). A-839977 inhibits BzATP-induced YO-PRO dye uptake, a marker of membrane pore formation, and IL-1β release from THP-1 cells (IC50s = 6.6 and 37 nM, respectively). In vivo, A-389977 (30, 100, and 300 µmol/kg, i.p.) reduces thermal hyperalgesia in rats. A-389977 (40 mg/kg) reduces thermal and mechanical hyperalgesia in a rat MRMT-1 mammary carcinoma model of cancer-induced bone pain.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Honore, P., Donnelly-Roberts, D., Namovic, M., et al. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice. Behav. Brain Res. 204(1), 77-81 (2009).

    2. Falk, S., Schwab, S.D., Frøsig-Jørgensen, M., et al. P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience 291, 93-105 (2015).