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

A-317491 sodium salt hydrate 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 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate 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 sodium salt hydrate Chemical Structure

A-317491 sodium salt hydrate Chemical Structure

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
USD 163 In-stock
Solution
10 mM * 1 mL in Water USD 163 In-stock
Solid
5 mg USD 122 In-stock
10 mg USD 182 In-stock
50 mg USD 617 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of A-317491 sodium salt hydrate:

Top Publications Citing Use of Products

    A-317491 sodium salt hydrate purchased from MedChemExpress. Usage Cited in: Int J Nanomedicine. 2017 Nov 9;12:8171-8183.  [Abstract]

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A-317491 sodium salt hydrate 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 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux[1][2].

    IC50 & Target

    P2X3 Receptor

     

    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].

    MedChemExpress (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].

    MedChemExpress (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

    606.57

    Formula

    C33H29NNaO9

    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O.[Na].O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (164.86 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6486 mL 8.2431 mL 16.4861 mL
    5 mM 0.3297 mL 1.6486 mL 3.2972 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 50 mg/mL (82.43 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.88%

    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 (sealed storage, away from moisture). 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
    H2O 1 mM 1.6486 mL 8.2431 mL 16.4861 mL 41.2154 mL
    5 mM 0.3297 mL 1.6486 mL 3.2972 mL 8.2431 mL
    10 mM 0.1649 mL 0.8243 mL 1.6486 mL 4.1215 mL
    15 mM 0.1099 mL 0.5495 mL 1.0991 mL 2.7477 mL
    20 mM 0.0824 mL 0.4122 mL 0.8243 mL 2.0608 mL
    25 mM 0.0659 mL 0.3297 mL 0.6594 mL 1.6486 mL
    30 mM 0.0550 mL 0.2748 mL 0.5495 mL 1.3738 mL
    40 mM 0.0412 mL 0.2061 mL 0.4122 mL 1.0304 mL
    50 mM 0.0330 mL 0.1649 mL 0.3297 mL 0.8243 mL
    60 mM 0.0275 mL 0.1374 mL 0.2748 mL 0.6869 mL
    80 mM 0.0206 mL 0.1030 mL 0.2061 mL 0.5152 mL
    100 mM 0.0165 mL 0.0824 mL 0.1649 mL 0.4122 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    A-317491 sodium salt hydrate Related Classifications

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    • 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-317491 sodium salt hydrate
    Cat. No.:
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