pparδ

GW9662 (TIMTEC-BB SBB006523) is a specific PPARγ antagonist (IC50: 3.3 nM, in a cell-free assay), with 100 to 1000-fold functional selectivity for PPARγ than PPARα δ in cells.

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

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.

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%.

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.

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 an insulin sensitizing agent and thiazolidinedione indicated for the treatment of type 2 diabetes, and has been linked to rare instances of acute liver injury.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.

Sakuranetin, a flavanone phytoalexin from ultraviolet-irradiated rice leaves, it has antifungal, antimutagenic, anti-inflammatory and antioxidant effects

Tesaglitazar is a potent and selective peroxide PPARα γ receptor dual agonist with a more potent affinity for PPARγ than PPARα, The EC50 values for rat PPARα and human PPARα were 13.4 μM and 3.6 μM, respectively, and 0.2 μM for rat PPARγ and human PPARγ. Tesaglitazar induced DNA synthesis and fibrosarcoma formation in rat subcutaneous mesenchymal cells.

Muraglitazar (BMS-298585) is a PPAR α γ dual agonist for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα and PPARγ with EC50 of 320 nM and 110 nM respectively.

MCC-555 (Isaglitazone) is a PPARα and PPARγ agonist exerting antihyperglycemic effects.

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

Linotroban(CL-871502) is a potent selective thromboxane (TXA2) receptor antagonist with antithrombotic activity.