a a A on s s Targeting PPARs: oac a o s Pha mace ca A on s s o e esso s An a on s s/Pa a A on s s A guide to function and structure PPAR α, δ, γ R R While PPARs display a high degree of homology at the protein level, each subtype exhibits distinct, noninter- changeable roles in energy metabolism that range from energy burning to energy storage. Learn more about A n n n e a e ene ansc on their functions as fatty acid sensors and regulators of energy homeostasis at www.caymanchem.com/PPARs. www.caymanchem.com oma n e on an n n oma n A A A/ MUSCLE PPARδ PPARα P s e · ↑ Fatty acid oxidation · ↑ Fatty acid oxidation · ↑ Oxidative muscle fibers · ↑ Obesity resistance PPARγ PPARα* PPARδ PPARγ* · ↑ Insulin-mediated · ↑ Insulin sensitivity glucose uptake A/ A/ A/ · ↑ Energy uncoupling Re esen s so o m he canon ca se ence n n P o Re esen s so o m he canon ca se ence n n P o
FAAR NR1C2 Synonyms NR1C1 NR1C3 NUC1 LIVER PPARα PPARγ PPARβ · ↑ Fatty acid oxidation · ↑ Fatty acid storage · ↑ Ketogenesis · ↑ Lipogenesis CREBBP EP300 · ↓ Plasma triglycerides CITED2 FAM120B CREBBP MED1 (PBP/DRIP205/TRAP220) · ↑ Plasma HDL EP300 EP300 NCOA1 (RIP160/SRC-1) NCOA1 (RIP160/SRC-1) MED1 (PBP/DRIP205/TRAP220) NCOA2 (SRC-2) NCOA2 (SRC-2) Coactivators NCOA1 (RIP160/SRC-1) NCOA3 (SRC-3) NCOA3 (SRC-3) NCOA2 (SRC-2) NCOA4 PGC-1α NCOA3 (SRC-3) NCOA6 PGC-1α NCOA7 VESSEL WALL PPARα & PPARγ PGC-1β PGC-1α · ↓ Inflammation PRIC295 PGC-1β · ↑ Reverse cholesterol transport PGC-2 NCOR1 GPS2 PPARδ NCOR1 NR0B2 PER2 NCOR1 · ↓ Inflammation Corepressors RIP140 (NRIP1) RIP140 (NRIP1) RIP140 (NRIP1) NR0B1 SMRT (NCOR2) SMRT (NCOR2) SMRT (NCOR2) NR0B2 SPEN
AM3102 Amorfrutin A Clofibrate Amorfrutin B WHITE ADIPOSE TISSUE PPARγ (+)-Etomoxir (sodium salt) Azelaoyl PAF · ↑ Adipogenesis Fenofibrate CAY10599 GW 590735 CAY10592 CDDO · Regulates adipokine production Selective Agonists GW 7647 GW 0742 Ciglitazone · ↑ Lipid repartitioning to fat GW 9578 GW 501516 GW 1929 8(S)-HETE Pioglitazone · ↑ Insulin sensitivity 12,14 Leukotriene B4 15-deoxy-Δ -Prostaglandin J2 · ↑ Lipogenesis N-Octadecyl-N’-propyl-sulfamide Rosiglitazone Oleoyl Ethanolamide Troglitazone
Bavachinin (±)13-HODE Bavachinin Lanifibranor Bezafibrate Lanifibranor Bezafibrate Bavachinin MHY908 Non-Selective and CAY10514 MHY908 Elafibranor CAY10514 BROWN ADIPOSE TISSUE PPARδ Bezafibrate Muraglitazar Dual Agonists CAY10573 Muraglitazar Lanifibranor CAY10573 · ↑ Fatty acid oxidation CAY10573 Tesaglitazar Elafibranor Tesaglitazar (±)9-HODE Wy 14643 · ↑ Energy uncoupling (±)9-HODE Wy 14643 (±)13-HODE
PPARγ BADGE GW 9662 Partial Agonists GSK3787 Diclofenac MCC-555 · ↑ Adipogenesis GW 6471 and Antagonists Sulindac FMOC-L-Leucine SR 202 G3335 T0070907