GW0742
Catalog No.S8020
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.
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.
Purity & Quality Control
Choose Selective PPAR Inhibitors
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. | ||||||||||||||||||||||||||||||
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| Features | Both GW0742 and L-165041 activate PPARβ, but not PPARγ or PPARα in platelets. | ||||||||||||||||||||||||||||||
| Targets |
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| 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] |
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| Cell Data |
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| 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] |
Protocol
| Cell Research:[2] |
+ Expand
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| Animal Research:[4] |
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Solubility (25°C)
| In vitro | DMSO | 94 mg/mL (199.36 mM) |
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| 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. |
3mg/mL |
* 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 |
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| Formula | C21H17F4NO3S2 |
| CAS No. | 317318-84-6 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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