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 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.
|Incubation time||24 h|
|Animal models||Homozygous obese (Ob) Zucker rats model of partial (~70%) hepatic warm ischemia|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
PPARα Agonist WY-14643 Induces SIRT1 Activity in Rat Fatty Liver Ischemia-Reperfusion Injury.
Pantazi E, et al. Biomed Res Int. 2015;2015:894679. PMID: 26539534.
PPARalpha activators inhibit cytokine-induced vascular cell adhesion molecule-1 expression in human endothelial cells.
Marx N, et al. Circulation. 1999 Jun 22;99(24):3125-31. PMID: 10377075.
|Related PPAR Products|
Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.
All-trans retinoic acid (ATRA; Vitamin A acid) has been widely investigated for treatments of many cancers including prostate cancer.
Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes.
Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.
Clofibrate (Atromid-S), a fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia.
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