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.

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.

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)).

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

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%.

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).

PPARδ agonist 9 (compound 21), with an EC50 of 3.6 nM, effectively decreases serum MCP-1 concentrations in mice and significantly reduces atherosclerotic development in the LDLr-KO model with a 50-60% inhibition rate in vivo [1].

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

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

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

Pparδ agonist 2 is an agonist of PPARδ.

Pparδ agonist 7 is a potent agonist of Pparδ, a member of the peroxisome proliferator-activated receptor (PPAR) intranuclear receptor transcription factor superfamily, which regulates metabolic homeostasis, inflammation, cell growth, and differentiation in vivo. [Tubulin aggregation-IN-19]

Pparδ agonist 8 is a potent activator of Pparδ, with potential applications in the study of nonalcoholic fatty liver disease (NAFLD).

Pparδ agonist 5 is a selective, orally active PPARδ agonist with an EC50 of 0.335 μM and better selectivity than GW0742. Pparδ agonist 5 has a beneficial effect on the improvement of bone density and microarchitecture in vivo.

Pioglitazone (U 72107) is a PPARγ agonist with EC50 of 0.93 and 0.99 μM on human and mouse PPARγ, respectively, and has selective and oral activity. Pioglitazone can be used in diabetes research.