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    InvivoChem Cat #: V0832
    CAS #: 317318-84-6Purity ≥98%

    Description: GW0742 (GW-0742; GW 0742; GW-0742X; GW0742X; GW610742; GW-610742) is a potent and highly selective PPARβ/δ agonist with potential anti-inflammatory activity. It acts by activating PPAR with an IC50 of 1 nM, and exhibits >1000-fold selectivity for PPARβ/δ  over PPARα and PPARγ.

    References: Bioorg Med Chem Lett. 2003;13(9):1517-21; Cell Signal. 2007;19(6):1163-71; Clin Transl Sci. 2009;2(2):127-33.

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    Molecular Weight (MW)471.49
    CAS No.317318-84-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 94 mg/mL (199.4 mM)
    Water: <1 mg/mL
    Ethanol: 44 mg/mL (93.3 mM)
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL  
    SynonymsGW-0742X; GW-610742; GW0742; GW-0742; GW 0742X; GW610742; GW 0742; GW0742X; GW 610742 

    Chemical Name: [4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methyl phenoxy]-acetic acid


    InChi Code: InChI=1S/C21H17F4NO3S2/c1-11-7-14(4-6-17(11)29-9-19(27)28)30-10-18-12(2)26-20(31-18)13-3-5-15(16(22)8-13)21(23,24)25/h3-8H,9-10H2,1-2H3,(H,27,28)

    SMILES Code: O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C(F)=C3)S2)C=C1C           

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    In Vitro

    In vitro activity: GW0742 shows activity aganist hPPARα, hPPARγ and hPPARδ with EC50 of 1.1 μM, 2 μM and 1 nM, respectively, in cell based transactivation assay. GW0742 (0.2 μM and 1 μM) significant increases in reporter activity of PPARβ/δ in N/TERT-1 keratinocytes. GW0742 (1 μM) results in significant inhibition in the average number of N/TERT-1 keratinocytes. GW0742 (1 μM) results in an increase in the number of cells in the G1 phase and a decrease in the number of cells in the S phase. GW0742 (1 μM) causes a significant increase in the mRNA encoding ADRP, a known PPARβ/δ target gene, in N/TERT-1 keratinocytes as well as mouse primary keratinocytes. GW0742 (1 μM) results in significantly reduced phosphorylation of retinoblastoma (Rb) and a significantly lower level of p42/44 ERK in N/TERT-1 cells. GW0742 (1 μM) leads to an increase in the mRNA encoding a number of known markers of terminal differentiation including TG-I, SPR1A, K10 and involucrin. GW0742 at 100 μM produces a significant reduction in low-KCl-induced neuronal cell death in cerebellar granule neurons. GW0742 at 100 μM induces a pronounced increase in cell death as measured by LDH release after 48 hr of incubation. GW0742 at 100 μM produces a pronounced increase in c-Jun expression at 6 hours in cerebellar granule neuron cultures. GW0742 at 100 μM increases PPARα-mediated transactivation dependent on the presence of 1.5% BSA in MCF-7 cells.

    Kinase Assay: GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

    Cell Assay:  N/TERT-1 keratinocytes are seeded onto 6-well tissue culture dishes at 3×104 cells per well in Ker-SFM. Twenty-four hours later, cell number is measured with a Z1 coulter particle counter to determine plating efficiency (Day 0). For the remaining cells, medium is changed to Ker-SFM/DF-K, and cells are treated in triplicate with 0.1% DMSO, 0.1 μM or 1 μM GW0742. Cell number is determined at daily intervals, and the remaining cells are retreated with fresh media and treatment each day for up to 6 days.

    In VivoGW0742 (10 mg/kg) promotes reverse cholesterol transport in C57BL6/J mice. GW0742 (10 mg/kg) increases the fecal excretion of HDLderived cholesterol despite no effect on HDL cholesterol catabolism in C57BL6/J mice. GW0742 decreases NPC1L1 mRNA expression in the small intestine of mice. GW0742 (30 mg/kg), prior to induction of LPS-mediated pulmonary inflammation, results in a significant decrease in leukocyte recruitment into the pulmonary space in Male BALB/c mice. GW0742 (30 mg/kg) significantly decreases protein and mRNA levels of the pro-inflammatory cytokines IL-6, IL-1beta and TNFalpha in Bronchial alveolar lavage fluid of mice. 
    Animal modelWild-type C57BL/6 female mice
    Formulation & DosageDissolved in saline; 10 mg/kg; Supplemented chow diet
    ReferencesBioorg Med Chem Lett. 2003 May 5;13(9):1517-21; Cell Signal. 2007 Jun;19(6):1163-71; Clin Transl Sci. 2009 Apr;2(2):127-33.

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


    N/TERT-1 keratinocytes express a functional PPARβ/δ. (A) N/TERT-1 keratinocytes were cultured as described and transfected with 3X-PPRE luciferase and β-galactosidase reporter plasmids. Cell Signal. 2007 Jun;19(6):1163-71.


    Effect of GW0742 on mRNA encoding cell cycle regulators. An RNase protection assay was performed using RNA from N/TERT-1 keratinocytes cultured in either 0.1% DMSO or 1.0 μM GW0742 after 24, 48 or 72 hours. Cell Signal. 2007 Jun;19(6):1163-71.


    Effect of PPARβ/δ on serum deprivation and UV irradiation changes in cell growth in wild-type (+/+) and PPARβ/δ-null (-/-) primary keratinocytes. Cell Signal. 2007 Jun;19(6):1163-71. 


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