PPARγ Agonist

PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC₅₀s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.

Inolitazone hydrochloride hydrate (Efatutazone hydrochloride hydrate) is a novel PPARγ high-affinity agonist, with an EC₅₀ value one-fiftieth that of Rosiglitazone (HY-17386), and shows no inhibitory effect on RIE cells that do not express PPARγ. Inolitazone hydrochloride hydrate can be used in the research of cancer.

BMS711939 is a selective agonist for peroxisome proliferator-activated receptor α (PPAR α), with EC₅₀ of 4 nM and 4.5 μM, for human PPARα and human PPARγ. BMS711939 exhibits good pharmacokinetic characters in rats models. BMS711939 increases HDL cholesterol, reduces LDL cholesterol and triglycerides.

MBX-102 acid is a selective partial PPAR-γ agonist. MBX-102 acid binds highly to plasma proteins, mainly serum albumin. MBX-102 acid can be used to study type 2 diabetes.

MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC₅₀ being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC₅₀ values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ.

PPARγ agonist-23 (Compound 9) is an orally active PPARγ agonist with an EC₅₀ of 0.32 μM. PPARγ agonist-23 improves hepatic triglyceride levels, reduces scores of steatosis and hepatocellular ballooning, and decreases the total activity score of non-alcoholic steatohepatitis (NASH). PPARγ agonist-23 can be used for the research of non-alcoholic steatohepatitis.

EL244 is a dua Autotaxin (ATX) (IC₅₀ = 50 nM) inhibitor and PPARγ (IC₅₀ = 1.3 μM; K_d = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC₅₀ = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.

PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC₅₀s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy.

LJ570 is a PPARα/PPARγ dual agonist with EC₅₀s of 1.05 and 0.12 μM, respectively.

Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC₅₀ of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.

PPAR agonist 8 is an orally active pan-PPAR agonist, with K_D values of 0.576 μM, 2.06 μM and 1.45 μM for PPARα, PPARγ and PPARδ, respectively. PPAR agonist 8 upregulates the expression of ATP-binding cassette transporter A1 (ABCA1) and promotes cholesterol efflux. PPAR agonist 8 reduces plasma cholesterol levels, decreases cholesterol accumulation in the liver and cholesterol deposition in pancreatic islets, regulates glucose and lipid metabolism, and causes no side effects of weight gain and obesity. PPAR agonist 8 can be used in the research of type 2 diabetes, hepatic steatosis and pancreatic islet dysfunction.

Neoambrosin is a sesquiterpene lactone. Neoambrosin acts as a partial agonist of PPARγ and TRPA1 receptors, with no carbonic anhydrase inhibitory activity. Neoambrosin can be used in research on hypoglycemia, analgesia, anti-inflammation and anticancer effects.

Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.

Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC₅₀ values of 67 and 31 nM.

GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pK_i of 8.84 for human PPAR-γ, and pEC₅₀s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential.

AU403 is a potent, brain-penetrant, isoform-selective LXRβ/PPARδ dual agonist (EC₅₀ ≈ 45 nM for LXRβ and EC₅₀ ≈ 40 nM for PPARδ). AU403 is designed to bypass LXRα-driven hepatotoxicity. AU403 significantly improves cognitive functions and reduces amyloid-β plaque burden in 3xTg-AD mice. AU403 is a promising dual-acting agonist for the research of Alzheimer’s disease.