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

A-740003 

Cat. No.: HY-50697 Purity: 98.91%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
Estimated Time of Arrival: December 31
100 mg USD 136 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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

    IC50: 18 nM (rat P2X7 receptor), 40 nM (human 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].

    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].

    Molecular Weight

    474.55

    Formula

    C₂₆H₃₀N₆O₃

    CAS No.

    861393-28-4

    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)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2107 mL 1.0536 mL 2.1073 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 (5.27 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
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    KeyWords:

    A-740003 | A740003 | A 740003 | P2X Receptor | P2XRs | Inhibitor | inhibitor | inhibit

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    Product name:
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