PPARγ Agonist

Prostaglandin A1 is a dehydrated derivative of Prostaglandin E1. Prostaglandin A1 exhibits antiviral, anti-inflammatory, antitumor, neuroprotective, and antihypertensive activities. Prostaglandin A1 covalently binds to cysteine residues of target proteins through Michael addition, or activates pathways such as PPARγ and HSPs via transcriptional regulation. Prostaglandin A1 is used in research on Mayaro virus infection, stroke, Alzheimer's disease, neuroblastoma, melanoma, and severe gestational hypertension.

Fenofibric acid (Standard) is the analytical standard of Fenofibric acid. This product is intended for research and analytical applications. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM.

Muraglitazar (BMS-298585) is an orally active non-thiazolidinedione oxybenzylglycine dual-target PPARα/PPARγ agonist, with an IC₅₀ of 0.25 μM and an EC₅₀ of 0.32 μM against human PPARα, and an IC₅₀ of 0.19 μM and an EC₅₀ of 0.11 μM against human PPARγ. Muraglitazar regulates lipid homeostasis, enhances peripheral insulin sensitivity, and improves β-cell function. Muraglitazar reduces levels of blood glucose, insulin, triglycerides and free fatty acids, normalizes adiponectin and corticosterone levels, promotes cholesterol efflux, reduces hepatic lipid content, regulates body weight, prevents hyperglycemia, and improves glucose tolerance. Muraglitazar can be used in research related to type 2 diabetes and dyslipidemia.

FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.

Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB₂ receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity.

MRL-24 is a PPARγ agonist. MRL-24 can be used in metabolic disease related research.

LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC₅₀=0.22 μm; mPPARα:EC₅₀=0.26 μm; hPPARγ:EC₅₀=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties.

ZLY06 is an orally active dual agonist of peroxisome proliferator-activated receptor (PPAR) δ and γ (PPAR δ: EC₅₀=341 nM; PPAR γ: EC₅₀=237 nM). ZLY06 induces hepatic lipid accumulation by inhibiting the phosphorylation of AKT1, mediating the upregulation of CD36. In addition, ZLY06 significantly improves glucose and lipid metabolism without increasing body weight, and alleviates fatty liver by promoting β-oxidation of fatty acids and inhibiting hepatic lipogenesis.

Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC₅₀s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC₅₀ of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.

10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [³H]Rosiglitazone for binding to PPAR-γ, with an IC₅₀ of 0.22 μM.