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    GW9508
    GW9508

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1805
    CAS #: 885101-89-3Purity ≥98%

    Description: GW9508 is a novel, potent and selective agonist for FFA1 (fatty acid receptor GPR40) with pEC50 of 7.32, and is 100-fold selective against GPR120, it stimulates insulin secretion in a glucose-sensitive manner. GW9508 is a GPR40/120 agonist and is different from the reported GPR40/120 agonist GW1100. When tested with HEK-293 (human embryonic kidney) cells expressing GPR40 or GRP120, GW9508 treatment increased intracellular Ca2+ concentration via activating GPR40/120 in a dose-dependent manner. 

    References: Br J Pharmacol. 2006 Jul;148(5):619-28; J Endocrinol. 2008 Sep;198(3):533-40.

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    Molecular Weight (MW)347.41
    FormulaC22H21NO3
    CAS No.885101-89-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 69 mg/mL (198.6 mM)
    Water: <1 mg/mL
    Ethanol: 69 mg/mL (198.6 mM)
    SynonymsGW9508; GW-9508; GW 9508.
    Other infoChemical Name: 3-(4-((3-phenoxybenzyl)amino)phenyl)propanoic acid
    InChi Key: DGENZVKCTGIDRZ-UHFFFAOYSA-N
    InChi Code: InChI=1S/C22H21NO3/c24-22(25)14-11-17-9-12-19(13-10-17)23-16-18-5-4-8-21(15-18)26-20-6-2-1-3-7-20/h1-10,12-13,15,23H,11,14,16H2,(H,24,25)
    SMILES Code: O=C(O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1


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    In Vitro

    In vitro activity: GW9508 is shown to be at least 100-fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ (pEC50 4.0, 4 and 4.9, respectively). GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). GW9508 dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, GW9508 is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. GW9508 induced hyperpolarization and opening of KATP channels in rat β-cells. GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes.


    Cell Assay: When tested with HEK-293 (human embryonic kidney) cells expressing GPR40 or GRP120, GW9508 treatment increased intracellular Ca2+ concentration via activating GPR40/120 in a dose-dependent manner. In rat pancreaticβ-cells, GW9508 treatment activated KATP channels which inhibited GSIS through agonist of GPR40 and GPR120. When tested with TNF-α treated rat L cells, administration of GW9508 increased the expression of GLP-2 via activating GPR40 and 120. 

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    ReferencesBr J Pharmacol. 2006 Jul;148(5):619-28; J Endocrinol. 2008 Sep;198(3):533-40.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    GW9508

    Pharmacological profile of the GW9508 and GW1100 at the GPR40 receptor. Br J Pharmacol. 2006 Jul;148(5):619-28.
     

    GW9508

    Effect of GW9508 and GW1100 on insulin secretion from the MIN6 mouse insulinoma cell line. Br J Pharmacol. 2006 Jul;148(5):619-28.
     

    GW9508

    Effect of KCl on GW9508-potentiatiation of insulin secretion. Potentiation of KCl-stimulated insulin secretion in the presence of GW9508 at 25 mM glucose. Br J Pharmacol. 2006 Jul;148(5):619-28.


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