Molecular Weight(MW): 471.49
GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
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(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.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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.|
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. 
|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.  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. |
-  Sznaidman ML, et al. Bioorg Med Chem Lett, 2003, 13(9), 1517-1521.
-  Burdick AD, et al. Cell Signal, 2007, 19(6), 1163-1171.
-  Smith SA, et al. J Neurosci Res, 2004, 77(2), 240-249.
|In vitro||DMSO||94 mg/mL (199.36 mM)|
|Ethanol||44 mg/mL (93.32 mM)|
|In vivo||30% propylene glycol, 5% Tween 80, 65% D5W||30 mg/mL|
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