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Encompassing Amino Acids: 166-468
Application: Screen for specific PPARα agonists.
Background: Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptors (NRs) that are important in cell differentiation and various metabolic processes, especially lipid and glucose metabolism. PPARα (Peroxisome proliferator-activated receptor alpha), also known as NR1C1 (nuclear receptor subfamily 1, group C, member 1) or PPARA, is activated by arachidonic acid and other polyunsaturated fatty acids and regulates the lipid metabolism in the liver, heart, and brown adipose tissue. Decreased expression of this protein is associated with several disorders: cardiovascular, neurodegenerative, and metabolic. In the last few decades, the therapeutic potential of their synthetic agonists on various metabolic diseases, including dyslipidemia, hyperglycemia, Type 2 Diabetes (T2D), as well as liver diseases, has been well-documented. Most recently, the US FDA approved PPARδ agonist Livdelzi® (seladelpar) for primary biliary cholangitis (PBC). This approval highlights the importance of the pharmacological actions of PPAR agonists.
Description: The PPARα (Peroxisome proliferator-activated receptor alpha)-GAL4 Luciferase Reporter HEK293 Cell Lineexpresses firefly luciferase under the control of the GAL4 upstream activation sequence (UAS). It has constitutive expression of human peroxisome proliferator-activated receptor α ligand binding domain (PPARα LBD, amino acids 166-468) fused to the DNA binding domain (DBD) of GAL4 (GAL4 DBD). This system allows specific measurement of the effect of PPARα agonists with low cross-reactivity from other nuclear receptors or from other PPAR isoforms.This cell line has been validated by stimulation with GW-7647, and for its lack of stimulation to Rosiglitazone and GW501516. Figure 1: Illustration of the mechanism leading to luciferase induction upon agonist treatment in PPARα (Peroxisome proliferator-activated receptor alpha)-GAL4 Luciferase Reporter HEK293 Cell Line.Interested in screening and profiling inhibitors, blocking antibodies, or activators of PPARa without the need to purchase and license the cell line?/ Check out our Cell Signaling Pathway Screening.
Host Cell Line: HEK293, Human Embryonic Kidney, epithelial-like cells, adherent.
Mycoplasma Testing: The cell line has been screened to confirm the absence of Mycoplasma species.
Storage Stability: Cells are shipped in dry ice and should immediately be thawed or stored in liquid nitrogen upon receipt. Do not use a -80°C freezer for long term storage.
Supplied As: Each vial contains ≥1 x 106 cells in 1 ml of Cell Freezing Medium (BPS Bioscience #79796)
Target: PPAR
Uniprot: Q07869
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: BSL-2
References: Berger, J. P., et al., 2005 Trends in Pharmacological Sciences 5: 244-251.Lin Y., et al., 2022 Front Endocrinol (Lausanne). 13: 1074911.
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