PPAR Agonist

15-LOX-IN-2 (Compound 2a) is an orally active COX-2/15-LOX inhibitor and a partial agonist of PPARγ. 15-LOX-IN-2 has anti-inflammatory activity and inhibits the levels of 20-HETE, IL-1β and TNF-α in RAW 264.7 cells treated with LPS (HY-D1056). In addition, 15-LOX-IN-2 has significant glucose uptake capacity in the absence of insulin. 15-LOX-IN-2 can be used for the research of metabolic diseases.

GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC₅₀ of 3 μM by using Ba²⁺ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrial membrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells.

PPARγ agonist 12 (compound 9i) is a potent and selective PPARγ agonist with EC₅₀s of 3.98 and 15.42 μM against PPARγ and PPARδ, respectively. PPARγ agonist 12 improves insulin secretion and has anti-diabetic effect.

KRP-101 is a compound that regulates the expression of genes related to lipid metabolism. It is a PPARα agonist that can highly sensitively regulate the expression of genes such as apolipoprotein A-IV, which may be related to lowering serum triglycerides and increasing HDL.

PPAR agonist 6 (compound 5a) is an agonist of PPAR with EC₅₀ values of 3.6 μM, 2.6 μM, and 2.7 μM for PPARα, PPARβ/δ, and PPARγ, respectively. PPAR agonist 6 represses the transactivation of the TNFα-dependent NF-κB-driven reporter in L929 cells.

GW0072 is a partial agonist of PPARγ and does not directly bind to the AF-2 helix of PPARγ, resulting in specific partial receptor transcriptional activation properties.

LY-510929 is a compound that induces left ventricular hypertrophy (LVH). Related studies have identified the relevant conditions in which LY-510929 may induce LVH by measuring multiple markers and using multiple techniques.

DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes.

PPARα agonist 1 is a potent and full hPPARα agonist.

VSP-77 is an orally active PPARγ agonist. VSP-77 selectively upregulates the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. VSP-77 significantly improves glucose tolerance, reduces fasting blood glucose and insulin levels in high-fat diet (HFD)-induced diabetic mouse models. VSP-77 can be used for the study of diabetes.

Rac-Pemafibrate-¹³C,d₃ (Rac-K13675-¹³C,d₃) is the deuterium and ¹³C-labeled Rac-Pemafibrate (HY-17618A). Pemafibrate racemate (K13675 racemate) is the racemate of pemafibrate, and activates PPARα activity, with EC₅₀s of 1 nM, >10 μM and 1.7 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively.

Ciprofibrate (Standard) is the analytical standard of Ciprofibrate. This product is intended for research and analytical applications. Ciprofibrate (Win35833) is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate acts as an orally active hypolipidaemic agent and can be used for the research of primary hyperlipidaemias.

K-111 (BM-170744) is an oral active PPAR alpha agonist. K-111 show efficacy in improving insulin resistance, reducing body weight, and ameliorating atherogenic dyslipidemia. K-111 can be used for study of type 2 diabetes, dyslipidaemia, obesity and the metabolic syndrome.

2'-Hydroxy-4-methoxychalcone is a PPARγ agonist. 2'-Hydroxy-4-methoxychalcone also exhibits inhibitory activity against gelatinase/collagenase and human glutathione S-transferase (GST), with an IC₅₀ of 5.2 μM and a K_i of 15.36 μM against GST. 2'-Hydroxy-4-methoxychalcone inhibits both the NF-κB and AP-1 signaling pathways, exerting anti-inflammatory activity; it also inhibits COX-2, conferring anti-cancer/anti-angiogenic activity. 2'-Hydroxy-4-methoxychalcone can be used in studies related to atherosclerosis, inflammatory diseases and cancer.

PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier.

PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with K_is of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes.

PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC₅₀: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%).

PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC₅₀, 4.34 μM).

PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC₅₀ values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent.

Oxeglitazar is an orally active compound that can be used for the research of type II diabetes.