PPAR Agonist

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

Norbixin is an orally active natural product with multiple activities such as retinal protection and oxidative stress regulation. Norbixin scavenges ROS, chelates metal ions, regulates plasmid and genomic DNA breakage, inhibits H₂O₂-induced mutagenesis, activates PPAR-α, modulates lipid levels, restores or regulates antioxidant enzyme activity, and alters NO levels. Norbixin prevents A2E accumulation and protects photoreceptor cells and retinal pigment epithelial cells. Norbixin is a derivative of Bixin (HY-N6884). Norbixin can be used in research related to diseases such as macular degeneration and diabetes, and also serves as a natural textile dye.

PPARα agonist 2 (compound 4u) is a potent and selective PPARα agonist with an EC₅₀ of 37 nM. PPARα agonist 2 exhibits >2,700-fold selectivity for PPARα over other PPAR isoforms. PPARα agonist 2 has the potential for retinal disorders research.

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.

Pparδ agonist 5, an orally active PPARδ-selective agonist (EC₅₀=0.335 μM), is much greater than that of the prototypical standard GW0742. Pparδ agonist 5 promotes improvements in bone density and microarchitecture in vivo.

Seladelpar Lysine dihydrate (MBX-8025 lysine dihydrate) is an orally active, selective PPAR-δ agonist with an EC₅₀ of 2 nM against hPPAR-δ. Seladelpar Lysine dihydrate reduces serum IL-31 and bile acid levels. It alleviates pruritus symptoms. Seladelpar Lysine dihydrate enhances insulin sensitivity, normalizes levels of hyperglycemia, hyperinsulinemia, glucose disposal capacity, serum lipids and hepatic free cholesterol. It reduces steatosis, hepatic inflammation and improves liver fibrosis. Seladelpar Lysine dihydrate reverses the pathological changes of non-alcoholic steatohepatitis (NASH). It is applicable to research related to primary biliary cholangitis and non-alcoholic steatohepatitis (NASH).

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.

Clofibric acid-d₄ is the deuterium labeled Clofibric acid (HY-B1415). Clofibric acid also is an herbicideClofibric acid (Chlorofibrinic acid) is an orally active PPARα agonist. Clofibric acid inhibits the fimbriation of Escherichia coli. Clofibric acid increases SOD activity. Clofibric acid lowers blood lipids and prevents experimental pyelonephritis. Clofibric acid has anticancer activity against ovarian cancer. Clofibric acid is also a herbicide. Clofibric acid is used in ovarian cancer, liver cancer, obesity, and urinary tract infection research.

Deutaleglitazar (Aleglitazar-d₂) is a agonist of dual peroxisome proliferatory activating receptor (PPARα and PPARγ).

GW 590735 sodium is a potent and selective PPARα agonist with activity in regulating lipid metabolism. GW 590735 significantly increased high-density lipoprotein (HDL) cholesterol, decreased low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL) cholesterol, and significantly reduced triglycerides. The maximum increases in HDL cholesterol for GW 590735 were 37%, 53% and 84%, respectively, compared with bezafibrate, torcetrapib and GW 590735.

PPARγ agonist 10 (compound 33g) is a PPARγ agonist, and stimulats the insulin secretion, glucose uptake and insulin Sensitivity in βTC6 Cells.

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.

Clofibric acid (Standard) is the analytical standard of Clofibric acid (HY-B1415). This product is intended for research and analytical applications. Clofibric acid (Chlorofibrinic acid) is an orally active PPARα agonist. Clofibric acid inhibits the fimbriation of Escherichia coli. Clofibric acid increases SOD activity. Clofibric acid lowers blood lipids and prevents experimental pyelonephritis. Clofibric acid has anticancer activity against ovarian cancer. Clofibric acid is also a herbicide. Clofibric acid is used in ovarian cancer, liver cancer, obesity, and urinary tract infection research.

PPARγ agonist 15 (Compound 7c) is an agonist for PPARγ. PPARγ agonist 15 inhibits the expression of alpha-amylase (HPA) and alpha-glucosidase (HLAG) with IC₅₀ of 28.35 µM and 26.21 µM. PPARγ agonist 15 enhances glucose uptake in the L6 myotube cell. PPARγ agonist 15 improves glucose homeostasis, insulin sensitivity, and lipid metabolism in rat Streptozotocin (HY-13753)-induced diabetes model.

Monascin (Standard) is the analytical standard of Monascin. This product is intended for research and analytical applications. Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist.

PPARα/δ agonist 2 (compound 14) is a potent PPARα and PPARδ agonist with EC₅₀s of 3255 nM and 1475 nM for human PPARα and PPARβ/δ, respectively. PPARα/δ agonist 2 shows anti-inflammatory effects.

PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib.

PPARδ agonist 12 (compound 25) is a PPARδ agonist that inhibits the production of inflammatory factors and nitric oxide. PPARδ agonist 12 can also effectively prevent macrophages from infiltrating inflammatory sites and can be used in inflammation research.

Bezafibrate-d₄ is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

SB-219994 is a peroxisome proliferator-activated receptors (PPARs) agonists. SB-219994 can inhibit airway neutrophilia and associated chemoattractants/survival factors. SB-219994 exhibits anti-inflammation effec.