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Agonist activity at Gal4-fused mouse PPAR-alpha ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay relative to control
Assay data:23 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at Gal4-fused mouse PPAR-alpha ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay
Assay data:18 Active, 23 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at mouse PPARalpha
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to recombinant human HSD17B10 assessed as shift in melting temperature by SYPRO orange dye based differential scanning fluorimetry assay
Assay data:1 Tested
Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of Pdk4 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis
Assay data:12 Active, 13 Tested
Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of Fgf21 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis
Assay data:9 Active, 13 Tested
Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of cd36 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis
Assay data:8 Active, 8 Tested
Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of fabp1 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis
Assay data:7 Active, 8 Tested
Inhibition of HSD17B10 (unknown origin) using estradiol as substrate incubated for 3 hrs and measured after 1 hr by NADH Glo luminescence assay
Assay data:15 Tested
SummaryRelated BioAssays by Target
Agonist activity at mouse PPARalpha transfected in Cos7 cells co-expressing with pBIND and pGL4.35 Gal4 UAS Luc reporter plasmid by measuring luciferase activity incubated for 16 hrs by luciferase reporter gene assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Surface Plasmon Resonance (SPR)Assay from US Patent US9346839: "Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's disease"
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
ABAD Enzymatic Activity Assay from US Patent US9346839: "Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's disease"
Assay data:5 Active, 1 Activity ≤ 1 µM, 8 Tested
Cell-Based Transcription Assay from Article 10.1124/jpet.108.143271: "Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist."
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Cell-Based Transcription Assay from Article 10.1021/jm800733h: "Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design."
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
In vivo agonist activity at PPARalpha in high fat diet-induced nonalcoholic steatohepatitis C57BL/6J mouse model assessed as increase in Cyp4a3 mRNA expression in liver administered at 100 mg/kg, po administered once daily for 7 days by quantitative real time PCR analysis
Assay data:1 Active, 1 Tested
In vivo agonist activity at PPARalpha in high fat diet-induced nonalcoholic steatohepatitis C57BL/6J mouse model assessed as increase in LPL mRNA expression in liver administered at 100 mg/kg, po administered once daily for 7 days by quantitative real time PCR analysis
In vivo agonist activity at PPARalpha in high fat diet-induced nonalcoholic steatohepatitis C57BL/6J mouse model assessed as increase in mACADM gene expression in liver at 100 mg/kg, po administered once daily for 7 days by quantitative real time PCR analysis
In vivo agonist activity at PPARalpha in high fat diet-induced nonalcoholic steatohepatitis C57BL/6J mouse model assessed as increase in mACADM gene expression in liver at 3 mg/kg, po administered once daily for 7 days by quantitative real time PCR analysis
Assay data:2 Active, 2 Tested
In vivo agonist activity at PPARalpha in high fat diet-induced nonalcoholic steatohepatitis C57BL/6J mouse model assessed as increase in mCPT1A gene expression in liver at 100 mg/kg, po administered once daily for 7 days and measured at >3 days by quantitative real time PCR analysis
In vivo agonist activity at PPARalpha in high fat diet-induced nonalcoholic steatohepatitis C57BL/6J mouse model assessed as increase in mCPT1A gene expression in liver at 3 mg/kg, po administered once daily for 7 days and measured at >3 days by quantitative real time PCR analysis
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