1. Membrane Transporter/Ion Channel
  2. P2X Receptor

A 839977 

Cat. No.: HY-13954 Purity: 98.05%
Handling Instructions

A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively).

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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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

    • Technical Information

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    • References

    Description

    A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). IC50 Value: Target: P2X7 in vitro: A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells [1]. in vivo: Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice [1].

    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

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

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

    Cat. No.: HY-13954