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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 178 In-stock
Solution
10 mM * 1 mL in DMSO USD 178 In-stock
Solid
1 mg USD 35 In-stock
5 mg USD 104 In-stock
10 mg USD 162 In-stock
50 mg USD 660 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

A 839977 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE A 839977

WB

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

    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.

    View All P2X Receptor Isoform Specific Products:

    View All Isoforms
    P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    A 839977 Related Antibodies

    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].

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

    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.
    Molecular Weight

    413.26

    Formula

    C19H14Cl2N6O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (241.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      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

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4198 mL 12.0989 mL 24.1978 mL 60.4946 mL
    5 mM 0.4840 mL 2.4198 mL 4.8396 mL 12.0989 mL
    10 mM 0.2420 mL 1.2099 mL 2.4198 mL 6.0495 mL
    15 mM 0.1613 mL 0.8066 mL 1.6132 mL 4.0330 mL
    20 mM 0.1210 mL 0.6049 mL 1.2099 mL 3.0247 mL
    25 mM 0.0968 mL 0.4840 mL 0.9679 mL 2.4198 mL
    30 mM 0.0807 mL 0.4033 mL 0.8066 mL 2.0165 mL
    40 mM 0.0605 mL 0.3025 mL 0.6049 mL 1.5124 mL
    50 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2099 mL
    60 mM 0.0403 mL 0.2016 mL 0.4033 mL 1.0082 mL
    80 mM 0.0302 mL 0.1512 mL 0.3025 mL 0.7562 mL
    100 mM 0.0242 mL 0.1210 mL 0.2420 mL 0.6049 mL
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    A 839977 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    A 839977870061-27-1A839977A-839977P2X ReceptorP2XRsInhibitorinhibitorinhibit

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