pparδ

Pparδ agonist 1 is an agonist of PPAR-δ(EC50 of 5.06 nM).

Pparδ agonist 2 is an agonist of PPARδ.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

T0070907(IC50=1 nM) , an effective and specific PPARγ inhibitor, with the >800-fold selectivity over PPARα and PPARδ.

KD-3010 (Kalypsys) is an orally active potent and selective PPARδ agonist for the study of liver injury.

Mavodelpar free acid hydrochloride (Pparδ agonist HCl) is a potent PPARδ agonist.

Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.

GW 501516 (Endurobol) is a effective and highly specifc PPARβ/δ agonist (EC50: 1 nM), with 1000-fold selectivity over hPPARα/γ.

Chiglitazar is a PPAR α/γ/δ agonist and insulin sensitizer used in the treatment of type 2 diabetes mellitus to lower blood glucose, regulate blood lipids, and have anti-inflammatory and anti-fibrotic effects.

Fonadelpar is an agonist of PPARδ. It also is used in the research of neuroparalytic keratopathy.

GW 7647 is an effective and highly selective PPARα agonist, the EC 50 values of human PPARα, PPARγ and PPARδ receptors are 6,1100 and 6200 nM, respectively. GW 7647 can reduce the production of nitric oxide in macrophages and has lipid-lowering and anti-inflammatory properties in the body.

Indeglitazar (PPM 204) is orally available pan-agonist of PPAR (PPAR subtypes alpha (α), delta (δ), and gamma (γ)).

MA-0204 is a highly selective and orally available peroxisome proliferator-activated receptor δ (PPARδ) modulator (EC50s: 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively). It is a potential treatment for Duchene Muscular Dystrophy (DMD).

GSK3787 is a specific and irreversible PPARδ inhibitor(pIC50= 6.6).

FH535, a Wnt/β-catenin signaling and PPAR inhibitor, exhibits anti-tumor activities.

GSK0660 is an antagonist and inverse agonist of PPARβ/δ.

Bocidelpar is a modulator of PPARδ with an EC50 of 7.80 nM and improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy muscle cells.

Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

Seladelpar (MBX 8025) has been used in trials studying the treatment of Hyperlipidemia.

GW0742 (GW610742) is an effective and specific PPARδ agonist (EC50: 1 nM/1.1 μM/2 μM, for human PPARδ/α/γ).

(E/Z)-Elafibranor ((E/Z)-GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.

Compound 11, a selective PPARδ agonist, demonstrates an EC50 of 20 nM, indicating its high affinity for PPARδ receptors. This compound efficiently reduces levels of nitric oxide (NO), as well as the pro-inflammatory cytokines TNFα and IL-6 in LPS-stimulated RAW264.7 cells via the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, Compound 11 exhibits remarkable stability in human liver microsomes and plasma. It significantly ameliorates foot edema induced by Carrageenan, displaying favorable pharmacokinetic properties with a bioavailability of approximately 100%.

PPARδ agonist12 (compound 25) is a PPARδ agonist that inhibits the production of inflammatory factors and nitric oxide. Additionally, PPARδ agonist12 effectively prevents macrophage infiltration into inflamed areas, making it useful for inflammation research.

Dual FXR/PPARδ agonist-2 is a dual agonist for FXR and PPARδ, derived from the hybridization of the FXR agonist GW-4064 and the PPARδ agonist GW-0742. It exhibits potent dual-target activity, with an EC50 of 12.28 nM for FXR activation and a 69% activation rate of PPARδ at a concentration of 100 nM. Additionally, dual FXR/PPARδ agonist-2 demonstrates antifibrotic effects in a mouse model of pulmonary fibrosis.