For research use only.

Catalog No.S8020

6 publications

GW0742 Chemical Structure

CAS No. 317318-84-6

GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.

Selleck's GW0742 has been cited by 6 publications

3 Customer Reviews

  • (b) Western blotting used to analyze the expression of caspase-12. The caspase-12 levels were quantified and normalized to the GAPDH levels (n=6; F=23.785>F0.01(3, 20); ∗∗P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (c) Western blotting used to analyze the ratio of cleaved caspase-3 to caspase-3 of the different groups (n=4; F=10.419>F0.01(3, 12); ∗∗P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey's multiple comparisons test. The data are presented as the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787

    Neuropharmacology, 2016, 113(Pt A):396-406. . GW0742 purchased from Selleck.

    Immunohistochemistry for α-SMA (green), Smemb (red), and DAPI (blue) in cerebral VSMC at 24 hours after Hb incubation.

    Sci Rep, 2017, 7:45234. GW0742 purchased from Selleck.

  • 16HBECs pretreated with SB216763 (10 μM, 4 h), SB203580 (10 μM, 30 min), GW0742 (1 μM, 30 min), or pre-transfected with negative control/β-catenin siRNA (50 nM, 24 h) were exposed to CSE for 24 h. The protein levels of PPARδ, phosphorylated and total p38 MAPK and phosphorylated and total ERK MAPK were detected by western blot.

    Lab Invest, 2016, 96(2):218-29. GW0742 purchased from Selleck.

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Biological Activity

Description GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
Features Both GW0742 and L-165041 activate PPARβ, but not PPARγ or PPARα in platelets.
PPARδ [1]
1 nM(EC50)
In vitro

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. [1] 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. [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CV-1 cells MYHGeY5kfGmxbjDhd5NigQ>? NEPWNVUzPCCq NUXDXXNGSWexbnnzeEBi[3Srdnn0fUBifCCvb4Xz[UBRWEGULXHsdIhiKGW6cILld5Nm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXi1zIHPlcIx{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? M4r2PFIyODd2NEOy
HEK293 cells MXrGeY5kfGmxbjDhd5NigQ>? MlHYWJJidnOjY4TpeoF1cW:wIH;mJHBRSVKmZXz0ZUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBRTEt2LWDQVmUh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NYW1cXRZOjN{N{O1NVk>
C2C12 cells MV3GeY5kfGmxbjDhd5NigQ>? NEf5PFE1KGSjeYO= MnPjRYdwdmm|dDDhZ5Rqfmm2eTDheEBRWEGUZHXseIEhcW5ibX;1d4UhSzKFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgeZBz\We3bHH0bY9vKG:oIGTGRW0h\2WwZTDlfJBz\XO|aX;uJIFnfGW{IESg[IF6eyCkeTDy[YFtKHSrbXWgVGNTKGGwYXz5d4l{ Mk\SNlMzPzN3MUm=

... Click to View More Cell Line Experimental Data

In vivo GW0742 (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. [4] 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. [5]


Cell Research:[2]
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  • Cell lines: N/TERT-1 keratinocytes
  • Concentrations: ~1 μM
  • Incubation Time: 6 days
  • Method: 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.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Wild-type C57BL/6 female mice
  • Dosages: 10 mg/kg
  • Administration: Supplemented chow diet
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (199.36 mM)
Ethanol 44 mg/mL (93.32 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 471.49


CAS No. 317318-84-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC(=C(C=C3)C(F)(F)F)F)C)OCC(=O)O

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID