GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. GW6471 (0.001-10 μM) disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. GW6471 adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes. GW6471 (10 μM) significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα. GW6471 (10 μM) abolishes the effect of fenofibrate (10 μM) or PPARα agonist WY14643 (50 μM), which raise levels of eNOS, NO, and BH4 in human umbilical vein endothelial cells.
Ecotoxicol Environ Saf. 2023 Nov 16;268:115711.
Mitochondrial dysfunction and endoplasmic reticulum stress induced by activation of PPARα leaded testicular to apoptosis in SD rats explored to di-(2-ethylhexyl) phthalate (DEHP)
GW6471 purchased from AbMole
| Molecular Weight | 619.67 |
| Formula | C35H36F3N3O4 |
| CAS Number | 880635-03-0 |
| Solubility (25°C) | DMSO 60 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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