1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. A 438079

A 438079 

Cat. No.: HY-15488 Purity: 99.64%
Handling Instructions

A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

For research use only. We do not sell to patients.

A 438079 Chemical Structure

A 438079 Chemical Structure

CAS No. : 899507-36-9

Size Price Stock Quantity
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 559 In-stock
Estimated Time of Arrival: December 31
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Other Forms of A 438079:

Top Publications Citing Use of Products

    A 438079 purchased from MCE. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401.

    Western analysis of protein expression levels in the treatment of compounds such as A 438079.

    A 438079 purchased from MCE. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401.

    Immunohistochemistry staining analysis of effects of rHSP90 and A438079 on neurobehavior and neurogenesis 48 h after SAH.
    • Biological Activity

    • Protocol

    • Technical Information

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    • References

    Description

    A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

    IC50 & Target

    pIC50: 6.9 (P2X7 receptor)

    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[1].

    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[1]. 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)[2]. A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores[3]. Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model[4]

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 0.2 mg/mL (0.65 mM; Need ultrasonic)

    References
    Kinase Assay
    [1]

    Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1 and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+ concentrations are assessed in all of the cell lines using the Ca2+ chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 10-10 to 10-4 M. BzATP or ATP concentrations corresponds to the EC70 values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and fluorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC50 or pIC50 values are derived from a single curve fit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    To confirm A 438079 reach the brain after systemic administration, P10 rat pups are injected with 5 mg/kg A 438079 and killed either 10 min, 30 min, or 2 h later (n=4 per group). Blood samples are centrifuged at 1000×g for 10 min to isolate the plasma. Samples are analyzed using liquid chromatography-mass spectrometry (LC-MS/MS) by a service provider. Briefly, protein is precipitated from 50 μL aliquots of the individual plasma or brain tissue homogenate, and A 438079 is quantified by LC-MS/MS from a five-point standard curve.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    306.15

    Formula

    C₁₃H₉Cl₂N₅

    CAS No.

    899507-36-9

    SMILES

    ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Inquiry Information

    Product Name:
    A 438079
    Cat. No.:
    HY-15488
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    A 438079

    Cat. No.: HY-15488