1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. A 839977

A 839977 

Cat. No.: HY-13954 Purity: 98.74%
Handling Instructions

A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.

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

A 839977 Chemical Structure

A 839977 Chemical Structure

CAS No. : 870061-27-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
10 mg USD 162 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A 839977 purchased from MCE. Usage Cited in: Part Fibre Toxicol. 2018 Oct 19;15(1):39.

    Total proteins of BV2 cells are extracted, and the levels of P2X7, NF-κB, ERK and p38 signaling pathway molecules are analyzed via Western Blot.
    • Biological Activity

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    • References

    Description

    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1].

    IC50 & Target

    IC50: of 20 nM (human P2X7 receptor), 42 nM (rat P2X7 receptor), 150 nM (mouse P2X7 receptor)[1]

    In Vitro

    A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models[1].
    A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes[2].

    RT-PCR[2]

    Cell Line: Optic nerve astrocyte cells
    Concentration: 50 nM
    Incubation Time: 1 hour(pre-treatment)
    Result: Prevented the IL-1β priming in astrocyte cells
    In Vivo

    A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats[1].
    A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice[1].
    A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals[3].

    Animal Model: Male Sprague-Dawley, BALB/c mice and IL-1 (−/−) mice for CFA-induced chronic inflammatory
    Dosage: 30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice)
    Administration: Injection; pre-injected 30mins
    Result: Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1 (−/−) mice.
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (241.98 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4198 mL 12.0989 mL 24.1978 mL
    5 mM 0.4840 mL 2.4198 mL 4.8396 mL
    10 mM 0.2420 mL 1.2099 mL 2.4198 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (6.05 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Molecular Weight

    413.26

    Formula

    C₁₉H₁₄Cl₂N₆O

    CAS No.

    870061-27-1

    SMILES

    ClC1=C(Cl)C(N2N=NN=C2NCC3=CC=CC=C3OC4=NC=CC=C4)=CC=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    A 839977
    Cat. No.:
    HY-13954
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    A 839977

    Cat. No.: HY-13954