PPAR Agonist

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.

5-Aminosalicylic Acid-d₃ (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC₅₀ values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis.

Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. Icosabutate is an orally active engineered fatty acid and a dual FFAR1/FFAR4 (GPR40/GPR120) agonist with EC₅₀ values of 10 μM and 15.5 μM, respectively. Icosabutate acts as a partial agonist of PPAR-α, with an EC₅₀ of 208 nM. Icosabutate inhibits the arachidonic acid cascade and exhibits antioxidant and anti-apoptotic activities. Icosabutate can be used in the research of nonalcoholic steatohepatitis, metabolic dysfunction-associated steatohepatitis, and atherosclerosis.

PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC₅₀ values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes.