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Application: Screen for specific PPARγ agonists.
Background: Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptors (NRs) that are important in cell differentiation and various metabolic processes. PPARγ, also known as glitazone reverse insulin resistance receptor or NR1C3 (nuclear receptor subfamily 1, group C, member 3) or PPARG, has two isoforms. PPARγ1 is found in several tissues, while isoform 2 is normally restricted to the adipose tissue. It is involved in fatty acid storage and in the expression of hormones linked to glucose homeostasis. During 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 Livdelzi® (seladelpar) for primary biliary cholangitis (PBC). This approval highlights the importance of the pharmacological actions of PPAR agonists.
Description: The PPARγ (Peroxisome proliferator-activated receptor gamma)-GAL4 Luciferase Reporter HEK293 Cell Line expresses firefly luciferase under the control of the GAL4 upstream activation sequence (UAS). It has constitutive expression of human peroxisome proliferator-activated receptor γ ligand binding domain (PPARγ LBD, amino acids 173-475) fused to the DNA binding domain (DBD) of GAL4 (GAL4 DBD). This system allows specific measurement of the effect of PPARγ agonists with low cross-reactivity from other nuclear receptors or from other PPAR isoforms. This cell line has been validated by stimulation with Rosiglitazone, and for its lack of stimulation to GW7647 and GW501516.Figure 1: Illustration of the mechanism leading to luciferase induction upon agonist treatment in PPARγ (Peroxisome proliferator-activated receptor gamma)-GAL4 Luciferase Reporter HEK293 Cell Line.Interested in screening and profiling inhibitors, blocking antibodies, or activators of PPAR 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.Ahmadian M., et al., 2013 Nat. Med. 19 (5): 10.1038.
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