GSK3787 is a potent and selective PPARbeta/delta antagonist. GSK3787 displays no measurable affinity for PPARα or PPARγ in vitro (pIC50< 5). GSK3787 has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells. In addition, GSK 3787 acts in a dual role as a weak agonist and antagonist towards PPARγ. In vivo and in vitro analysis indicates that the efficacy of GSK3787 to modulate PPARgamma activity is markedly lower than the efficacy of GSK3787 to act as a PPARbeta/delta antagonist. GSK3787 antagonized GW0742-induced expression of Angptl4 in mouse fibroblasts, mouse keratinocytes, and human cancer cell lines.
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Source | Toxicol Lett (2015). Figure 1. GSK 3787 |
| Method | Cell viability assay | |
| Cell Lines | H9c2 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Similarly, addition of GSK 3787 reduced the cytotoxic effect of DHA toward cellular metabolic activity in H9c2 cells. |
| Molecular Weight | 392.78 |
| Formula | C15H12ClF3N2O3S |
| CAS Number | 188591-46-0 |
| Solubility (25°C) | DMSO 49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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