1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. A-740003

A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.

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

A-740003 Chemical Structure

A-740003 Chemical Structure

CAS No. : 861393-28-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mg USD 66 In-stock
50 mg USD 92 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A-740003 purchased from MedChemExpress. Usage Cited in: Purinergic Signal. 2017 Jun;13(2):215-225.   [Abstract]

    Effect of A-740003 on thermal pain thresholds and P2X7R expression following the neck incision and EA stimulation.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.

    IC50 & Target

    P2X7 Receptor

     

    In Vitro

    A-438079 or A-740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response[1]. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death[2]. A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A-740003 and A-438079 show greater activity at rat and human, as compared with mouse P2X7 receptors[3]. A-740003 potently blocks agonist-evoked IL-1β release with (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells[4].

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

    In Vivo

    Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat. A-740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED50=38-54 mg/kg i.p.). A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses[4].

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

    Molecular Weight

    474.55

    Formula

    C26H30N6O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N#C/N=C(NC(NC(CC1=CC(OC)=C(C=C1)OC)=O)C(C)(C)C)\NC2=CC=CC3=NC=CC=C23

    Shipping

    Room temperature in continental US; may vary elsewhere.

    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 : 50 mg/mL (105.36 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 2.1073 mL 10.5363 mL 21.0726 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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 (5.27 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    (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:
    %
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    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
    Animal Administration
    [4]

    The response to acute thermal stimulation is determined using a commercially available paw thermal stimulator. Rats are placed individually in Plexiglas cubicles mounted on a glass surface maintained at 30°C and allowed a 30-min habituation period. A thermal stimulus, in the form of radiant heat emitted from a focused projection bulb, is then applied to the plantar surface of each hind paw. In each test session, each rat is tested in three sequential trials at approximately 5-min intervals. Paw-withdrawal latencies (PWLs) are calculated as the median of the two shortest latencies. An assay cut off is set at 20.5 s. A-740003 is injected i.p. 30 min before testing for acute thermal pain.

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

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1073 mL 10.5363 mL 21.0726 mL 52.6815 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 mL 10.5363 mL
    10 mM 0.2107 mL 1.0536 mL 2.1073 mL 5.2681 mL
    15 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5121 mL
    20 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6341 mL
    25 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
    30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7560 mL
    40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3170 mL
    50 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0536 mL
    60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
    80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
    100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
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    A-740003 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.

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    Product Name:
    A-740003
    Cat. No.:
    HY-50697
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