|
| Ligands | Receptor | Selective | Function |
|
| Saturated Fatty acid | PPAR-α
(liver, adipose tissue, kidney, heart, skeletal, muscle, large intestine) | Endogenous lipid with PPAR-α agonist active | Lipid and glucose metabolism |
| Unsaturated Fatty acid | Endogenous lipid with PPAR-α agonist active | Lipid and glucose metabolism |
| CP775146 | Selective, high affinity PPAR-α agonist | Lipid and glucose metabolism |
| Fenofibrate | PPAR-α agonist | Treatment of hypertriglyceridemia and dyslipidemia |
| GW7647 | Highly selective, potent PPAR-α agonist. Orally active | Lipid homeostasis, beta oxidation |
| Oleylethanolamide | PPAR-α agonist | Lowers body weight and hyperlipidemia |
| Palmitoylethanolamide | Endogenous lipid with PPAR-α agonist active | Anti-inflammatory, reduces pain |
| WY14643 | Selective PPAR-α agonist | Atherosclerosis and anti-inflammation and prevent hyperinsulinemia |
| GW6471 | Selective PPAR-α antagonist | Antagonist fenofibrates |
| MK886 | Selective PPAR-α antagonist | Inhibit PPAR-α, β, γ activities |
|
Fatty acids
(i) Docahexanoic acid
(ii) Arachidonic acid
(iii) Linolenic acid | PPAR-β
(Ubiquitous) | Endogenous lipid with PPAR-β agonist active | Anti-inflammation |
| GW501516 | Highly selective, potent PPAR-β agonist | Increases serum HDL-c in atherogenic dyslipidemia and decreases fasting blood sugar. |
| GW0742 | Potent PPAR-β agonist | Anti-inflammatory |
| L-165,041 | PPAR-β selective agonist | Hyperlipidemia, hyperglicemia, ateroesclerosis, and obesity |
| GW610742 | PPAR-β selective agonist | Treatment diabetic and nephropathy |
| FH535 | PPAR-β selective antagonist | Treatment diabetic and nephropathy |
| GSK0660 | PPAR-β selective antagonist | Inverse agonist PPAR-β/γ |
| GSK3787 | Potent and selective PPAR-β antagonist | Inverse agonist PPAR-β/γ |
| NSAIDs | PPAR-β selective antagonist | Cancer |
|
| Linolenic acid | PPAR-γ
(adipose tissue, lymphoid tissue, colon, liver, heart) | Endogenous lipid with PPAR-γ agonist active | Anti-inflammation |
| Arachidonic acid | Endogenous lipid with PPAR-γ agonist active | Anti-inflammation |
| 15d-PGJ2 | Endogenous lipid with PPAR-γ agonist active | Anti-inflammation |
| 9-HODE | Endogenous lipid with PPAR-γ agonist active | Anti-inflammation |
| 13-HODE | Endogenous lipid with PPAR-γ agonist active | Anti-inflammation |
| 15-HETE | Endogenous lipid with PPAR-γ agonist active | Anti-inflammation |
| Ciglitazone | Selective PPAR-γ agonist | Inhibits cell proliferation |
| GW1929 hydrochloride | Selective PPAR-γ. Orally active | Decreases glucose, fatty acids, and triglyceride |
| LG100754 | PXR:PPAR agonist | Sensitizes PPAR-γ |
| nTZDpa | PPAR-γ selective agonist | Anti diabetic, anti carcinogenic |
| JTT-501 (isoxazolidinedione) | PPAR-γ selective agonist | Anti diabetic |
| Pioglitazone hydrochloride | Selective PPAR-γ agonist | Anti diabetic |
| S26948 | Selective PPAR-γ agonist | Anti diabetic |
| Troglitazone | Selective PPAR-γ agonist | Anti diabetic |
| FH535 | PPAR-γ antagonist | Inhibits Wnt/β-catenin signaling |
| GSK0660 | PPAR-γ antagonist | Inverse agonist PPAR-β/γ |
| GSK3787 | PPAR-γ antagonist | Inverse agonist PPAR-β/γ |
| BADGE | PPAR-γ selective | Antagonist for roziglitazone |
| LG-100641 | PPAR-γ selective | Blocks TZDs antagonist |
|
