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Garcinolic acid

CHEMBL1456870

A Positive Modulator of P2X7 Receptors

Cat #: G-155
Alternative Name CHEMBL1456870
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Garcinia spp.
    Source Natural
    MW: 646.78
    Purity: >95%
    Effective concentration 10-100 µM.
    Structure
    Chemical name (4R)-4-[(2E)-3-carboxy-3-methylprop-2-en-1-yl]-14-hydroxy-6,6,18-trimethyl-21-(3-methylbut-2-en-1-yl)-18-(4-methylpent-3-en-1-yl)-12-oxo-2,5,19-trioxapentacyclo[11.8.0.0^{3,7}.0^{3,11}.0^{15,20}]henicosa-1(21),10,13,15(20),16-pentaene-4-carboxylic acid
    Molecular formula C38H46O9.
    PubChem CID 6857794
    Activity Garcinolic acid is a natural compound isolated from Garcinia resin, shown to facilitate and potentiate cellular responses mediated by the purinergic P2X7 receptors at over 10 µM1.
    References-Activity
    1. Fischer, W. et al. (2014) Purinergic Signal. 10, 313.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Soluble in DMSO, DMF and other organic solvents. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs Garcinolic acid activates human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs Garcinolic acid activates human P2X7 receptors expressed in HEK-293 cells.
      Dose response curve of hP2X7 activation by Garcinolic acid (#G-155). Cells were loaded with Fluo-8 NW dye, and stimulated with increasing concentrations of Garcinolic acid. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Fischer, W. et al. (2014) Purinergic Signal. 10, 313.
    2. Deng, Y.X. et al. (2012) Fitoterapia 83, 1548.
    3. Stokes, L. et al. (2006) Br. J. Pharmacol. 149, 880.
    Scientific background

    Garcinolic acid, a type of xanthone, is a positive modulator of the purinergic P2X7 receptors. It facilitates and potentiates cellular responses mediated by the purinergic P2X7 receptors at concentrations over 10 µM1,2.

    P2X receptors are ligand-gated cation-permeable channel complexes that are activated by extracellular ATP. This family contains seven subtypes: P2X1-P2X7 that can be assembled as trimeric complexes. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors are expressed in almost all tissues, particularly in cells of haematopoietic origin1,3.

    Target P2X7 receptors
    Lyophilized Powder
    Last update: 06/11/2022

    Garcinolic acid (#G-155) is a highly pure, natural, and biologically active compound.

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    For research purposes only, not for human use
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