WY 14643 is a highly potent PPARα agonist with EC50 values of 0.63, 32 and > 100 μM at PPARα, PPARγ and PPARδ respectively. PPARα is a subtype of PPAR, which controls the expression of genes involved in cardiac fatty acid utilization. Activated PPARs act as transcription factors to increase expression of specific genes within cells. In vitro, WY 14643 (Pirinixic Acid) inhibits NF-κB transcriptional activity and decreases the inflammatory response. And Pirinixic Acid inhibits the proliferation of trophoblast cells in vivo. MCD diet-induced fibrosing steatohepatitis can be reversed by treatment with WY-14643. WY 14643 may increase the progesterone secretion. Effects of WY-14643 on metabolism of human trophoblast cells are different from those of clofibric acid.
Cell Rep. 2019 Dec 17;29(12):4127-4143.e8.
SIRT6 Promotes Hepatic Beta-Oxidation via Activation of PPARα.
WY 14643 (Pirinixic Acid) purchased from AbMole
Cell Experiment | |
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Cell lines | U937 cells |
Preparation method | Adhesion Assay. ECs were grown to confluence in 96-well plates, pretreated with PPARα activators for 24 hours, and stimulated with TNF-α for 8 hours, then adhesion assays were performed.19 Briefly, U937 cells were labeled with 2',7'-bis(2-carboxy)-fluorescein acetoxymethyl ester (Molecular Probes) and then added, under rolling conditions (63 rpm, 23°C, 15 minutes), to a rinsed EC monolayer (2×106 cells/mL) in RPMI medium/10% FCS/1 mmol/L CaCl2. Nonadherent cells were removed by inverting the plate under rotation (20 minutes). After solubilization of well contents, fluorescence intensity was measured in a microtiter plate fluorimeter (Pandex, FCA). A standard curve using dilutions of labeled U937 cells was determined, and results were expressed as cells/cm2. |
Concentrations | 250 µmol/L |
Incubation time | 24 h |
Animal Experiment | |
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Animal models | Homozygous obese (Ob) Zucker rats model of partial (~70%) hepatic warm ischemia |
Formulation | - |
Dosages | 10 mg/kg |
Administration | intravenously |
Molecular Weight | 323.8 |
Formula | C14H14ClN3O2S |
CAS Number | 50892-23-4 |
Solubility (25°C) | DMSO 65 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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