1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. A-317491

A-317491 

Cat. No.: HY-15568 Purity: 99.18%
Handling Instructions

A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.

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

A-317491 Chemical Structure

A-317491 Chemical Structure

CAS No. : 475205-49-3

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10 mM * 1 mL in DMSO USD 152 In-stock
Estimated Time of Arrival: December 31
5 mg USD 122 In-stock
Estimated Time of Arrival: December 31
10 mg USD 182 In-stock
Estimated Time of Arrival: December 31
50 mg USD 617 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of A-317491:

Top Publications Citing Use of Products

    A-317491 purchased from MCE. Usage Cited in: Int J Nanomedicine. 2017 Nov 9;12:8171-8183.

    PC12 cell fluorescence images of baseline (before ATP stimulation), 0 s (the brightest fluorescence images after ATP stimulation), 50 s, 100 s, 150 s, and 200 s. Ca2+ peak increase (∆F/F0) in PC12 cells incubated with A-317491 salt, CSOSA/NLC, and CSOSA/NLC/A-317491 for predetermined time under 100 μM ATP stimulation.
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    Description

    A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux[1][2].

    IC50 & Target

    Ki: 22 nM (hP2X3), 22 nM (rP2X3), 9 nM (hP2X2/3), 92 nM (rP2X2/3)[1]

    In Vitro

    A-317491 potently blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki=22-92 nM) [1].
    A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC50 of 15 nM[1].

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

    In Vivo

    A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats[2].
    A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg)[2].

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

    Animal Model: Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant[2]
    Dosage: 0.1, 1, 3, 10, 30 mg/kg
    Administration: A single s.c.
    Result: Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.
    Molecular Weight

    565.57

    Formula

    C₃₃H₂₇NO₈

    CAS No.

    475205-49-3

    SMILES

    O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[[email protected]]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O

    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 : ≥ 47 mg/mL (83.10 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 1.7681 mL 8.8406 mL 17.6813 mL
    5 mM 0.3536 mL 1.7681 mL 3.5363 mL
    10 mM 0.1768 mL 0.8841 mL 1.7681 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 (4.42 mM); Clear solution

    • 2.

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

      Solubility: 2.5 mg/mL (4.42 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

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

    A-317491A317491A 317491P2X ReceptorP2XRsP2X3P2X2/3inflammatoryneuropathicpaincalciumfluxInhibitorinhibitorinhibit

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    Product Name:
    A-317491
    Cat. No.:
    HY-15568
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