Molecular Weight(MW): 392.78
GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
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PPARβ/δ activation protects against corticosterone-induced astrocyte damage. (a) Astrocytes treated with Cort at concentrations of 1, 10, and 100 μM( n = 4; F = 329.412 > F0.01 (3, 12); **P < 0.01 vs. Con group); (b) MTT assay performed 24 hours after treatment with Cort (10 μM) and GW (0.1, 1, and 10 μM) (n = 5; F = 7.402 > F 0.01 (4, 20); **P < 0.01 vs. Con group; #P < 0.05 vs. Cort. group); (c) MTT assay performed after 24 hours of treatment with Cort (10 μM), GW (10 μM), and GSK (10 μM) (n = 4; F = 42.431 > F0.01 (3, 12); **P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (d) MTT assay performed 24 hours after treatment with GSK (0.1, 1, and 10 μM) (n = 4; F = 1.659 < F0.01 (3, 12); P > 0.05 vs. Con group); (e) PPARβ/δ expression levels measured by RT-qPCR (n = 4; F = 27.018 > F0.01 (3, 12); **P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group); (f) PPARβ/δ expression levels measured by Western blot (n = 4; F = 34.723 > F0.01 (3, 12); **P < 0.01vs. Con group; ##P < 0.01 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey’s multiple comparisons test. Each data point represents the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787.
Neuropharmacology, 2017, 113(Pt A):396-406. GSK3787 purchased from Selleck.
(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. . GSK3787 purchased from Selleck.
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|Description||GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.|
GSK3787 irreversibly antagonizes human and mouse PPARδ that covalently modifies Cys249 within the ligand binding pocket. GSK 3787 completely antagonizes the activity of agonist GW501516 with a pIC50 of 6.9 and 94% maximal inhibition. GSK3787 (1 μM) effectively antagonizes the agonist GW0742 stimulated transcription of CPT1a and PDK4 in human skeletal muscle cells, and effectively antagonize the basal gene expression of CPT1a. GSK 3787 shows no effective antiproliferative activity against colorectal cancer cells.  GSK3787 (1 μM) completely antagonizes 50 nM GW0742-induced PPARβ/δ-dependent Angptl4 gene expression in wild-type fibroblasts and in keratinocytes. GSK3787 (1 μM) largely antagonizes 50 nM GW0742-induced Angptl4 and Adrp mRNAs expression in skin cancer cell A341. GSK3787 (1 μM) largely antagonizes GW0742-induced Angptl4 mRNAs expression in cancer cell lines MCF7 (breast), Huh7 (liver), and HepG2 (liver) cells but not in H1838 or A549 cells (lung). GSK3787 (1 μM) largely antagonizes GW0742-induced increase of Adrp mRNA in Huh7 and HepG2 cells but not in H1838 cells. GSK3787 does not antagonize basal expression of either of these two PPARβ/δtarget genes in these cells. Neither GW0742 nor GSK3787 has any effect on cell proliferation of these cells at concentrations ranging from 0.1 to 10 μM. GSK3787 is able to modulate the association of both PPARβ/δ and PPARγ coregulator peptides in response to ligand activation. Efficacy of GSK3787 to modulate PPARγ activity is markedly lower than the efficacy of GSK3787 to act as a PPARβ/δ antagonist. 
|In vivo||GSK3787 antagonizes ligand-induced PPARβ/δ-dependent gene expression in vivo. Oral administration of GSK3787 has no effect on the expression of Angptl4 and Adrp mRNA in mouse colon epithelium. Coadministration of GSK3787 (10 mg/kg) effectively prevents the GW0742-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, which is correlated with reduced promoter occupancy of PPARβ/δ on the Angptl4 and Adrp genes. Administration of GSK3787 had no effect on glucose tolerance. |
|In vitro||DMSO||79 mg/mL (201.13 mM)|
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