MA-0204 is a highly potent and selective PPARδ modulator (PPARδ EC50 = 0.4 nM; PPARα, EC50 = 6,660 nM) that upregulates the expression of FAO genes in human renal proximal tubule cells, resulting in increased mitochondrial fatty acid oxidation. MA-0204 is >10,000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. MA-0204 exhibits high protein binding to mouse plasma, good permeability and low potential for efflux. C.
In normal rats undergoing IR-AKI, MA-0204 attenuates the increases of plasma and urinary biomarkers of AKI, improves renal function, mitigates proximal tubular damage and boosts mitochondrial gene expression. PPARδ (30, 100 mg/kg) increases target gene transcription in the muscle.
| Molecular Weight | 476.49 |
| Formula | C25H27F3N2O4 |
| CAS Number | 2095128-17-7 |
| Solubility (25°C) | DMSO 39 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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