Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARdelta agonists.

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Luckhurst CA, Stein LA, Furber M, Webb N, Ratcliffe MJ, Allenby G, Botterell S, Tomlinson W, Martin B, Walding A

Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARdelta agonists.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. doi: 10.1016/j.bmcl.2010.10.117. Epub 2010 Oct 27.

PubMed ID

21094606 [ View in PubMed

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Abstract

Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor delta (PPARdelta. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cardarine	Peroxisome proliferator-activated receptor delta	EC 50 (nM)	2	N/A	N/A	Details