Biological Information

Background Information:

Peroxisomes proliferators include hypolipidemic drugs, leukotriene receptor antagonists and other materials. The term is used because they induce an increase in the size and number of peroxisomes, which are subcellular organelles found in animals and plants that contain enzymes for respiration and for cholesterol and lipid metabolism. The action of peroxisome proliferators is thought to be mediated via specific receptors, called PPARs, which belong to the steroid hormone receptor superfamily that function as transcription factors regulating the expression of genes. All PPARs heterodimerase with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. PPARs play essential roles in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein) of higher organisms. Three closely related subtypes (alpha, beta/delta, and gamma) have been identified. PPARA is expressed in liver, kidney, heart, muscle, adipose tissue, and others. PPARA is activated by leukotriene B4 as well as fibrate drugs .

PathHunter NHR Protein Interaction cell lines are engineered to co-express a ProLink™ (PK) tagged NHR and an Enzyme Acceptor (EA) tagged SRC protein. Activation of the receptor results in SRC-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

NHR

Sub Family:

Peroxisome Proliferator-Activated

Class:

Non-Steroid

Protein Name:

PPARalpha

Uniprot Number:

Q07869

Protein Aliases:

Nuclear receptor subfamily 1 group C member 1

Gene Name:

PPARA

Gene ID:

5465

Gene Aliases:

hPPAR|NR1C1

Accession Number:

NM_005036

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Testing Information

Control Activator:

GW7647

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

PPARA receptor agonism may be used to lower cholesterol (generally adjunctive to statins) and treat disorders that feature high triglycerides

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA