PPAR Agonist

20-HEPE is a metabolite of eicosapentaenoic acid formed by ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. At 10 μM, it activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter gene. 20-HEPE also activates mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks analgesic activity in rats.

PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib.

PPARα agonist 4 (compound BH400) is a PPARα agonist (EC₅₀= 1.2 μM). PPARα agonist 4 also inhibits STING (IC₅₀: 8.1 μM). PPARα agonist 4 reduces the CoCl₂-induced production of ROS and LPS-induced secretion of IL-6. The PPARα agonist 4 restores the decreased expression of PCG1α induced by LPS.

S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC₅₀=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ.

Anti-NASH agent 2 (compound 21) is an inhibitor of de novo adipogenesis activity and α-SMA gene expression. Anti-NASH agent 2 improves hepatic steatosis, edema, inflammatory infiltrates, and liver fibrosis in NASH mouse models.

PPAR agonist 7 is an orally active pan-PPAR agonist, demonstrating potent activation of all three subtypes, PPARα (EC₅₀ = 1.51 μM), PPARδ (EC₅₀ = 1.11 μM), and PPARγ (EC₅₀ = 3.14 μM). PPAR agonist 7 significantly enhances glucose uptake in adipocytes while exhibiting minimal adipogenic activity. PPAR agonist 7 can suppress PPARγ Ser273 phosphorylation in white adipose tissue and upregulate insulin-sensitizing genes. PPAR agonist 7 does not cause weight gain or fluid retention in high-fat diet (HFD)/ Streptozotocin (HY-13753) (STZ)-induced type 2 diabetes mellitus (T2DM) models. PPAR agonist 7 has selective modulation of PPAR signaling pathways without activation of adipogenic gene programs. PPAR agonist 7 can be used for the study of diabetes.

PPARγ agonist 20 is a potent, orally active PPAR-γ agonist. PPARγ agonist 20 effectively increases antioxidant defenses (SOD, GSH) and reduces lipid peroxidation. PPARγ agonist 20 can upregulate of Pparg, Glut4, and AdipoQ, suppresses of TNF-α, IL-6, and NF-κB p65. PPARγ agonist 20 significantly lowers fasting blood glucose, improving glucose tolerance, and restoring metabolic balance in Streptozotocin (HY-13753)-Nicotinamide (HY-B0150)-induced diabetic rats. PPARγ agonist 20 can be used for the study of type 2 diabetes.

PPARγ agonist 6 (Compound 12) is a potent and selective agonist of PPARγ. PPARγ agonist 6 has the potential for the research of cancer diseases.

Nor-LY-510929 is a compound whose development in the field of endocrinology and metabolism was stopped in 2005. Its specific active mechanism and application details are not described in detail based on the existing information.

Rivoglitazone hydrochloride (R-106056 hydrochloride) is a peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist. Rivoglitazone hydrochloride (R-106056 hydrochloride) exerts its anti-diabetic effect by activating PPARγ to regulate the expression of a large number of genes related to lipid and glucose metabolism. Rivoglitazone hydrochloride (R-106056 hydrochloride) can be used to study insulin secretion and insulin resistance in animal models of diabetes.

(R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease.

Halofenate, structurally akin to clofibrate, was evaluated in hypertriglyceridemic patients over 6-week periods in a controlled, double-blind crossover trial. It effectively reduced serum triglycerides by 50%, with minimal impact on serum cholesterol levels. Additionally, it lowered serum uric acid by 30% and exhibited uricosuric effects independent of glomerular filtration rate. Halofenate was associated with a significant increase in plasma thyroxine (T4), accompanied by a decrease in protein-bound iodine and T4 by column. In vitro studies confirmed its ability to displace T4 from thyroid-binding proteins, suggesting a thyroxine-displacing effect, which could influence thyroid function in vivo.

Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

L-764406 is a non-thiazolidinedione (TZD)-type PPARg nuclear receptor ligand with high affinity. L-764406 has significant binding ability to PPARg (IC₅₀=70 nM). L-764406 exhibited partial agonist activity and induced expression of the adipocyte-specific gene aP2 in chimeric receptors expressing the PPARg LBD and the corresponding reporter gene, as well as in 3T3-L1 cells. In contrast, L-764406 showed no activity in cells transfected with chimeric receptors containing PPARa or PPARd LBDs.

PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders.

SP-C01 is an orally active soluble epoxide hydrolase (sEH) inhibitor and partial PPARγ agonist. SP-C01 can inhibit Ser273 phosphorylation.

Ciprofibrate-d₆ is deuterium labeled Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha.

BR101549 is a non-TZD agonist of PPARγ. BR101549 activates PPARγ to the level of Pioglitazone in vitro. BR101549 can control blood glucose level in mouse model. BR101549 can be studied in anti-diabetic research.

Clofibrate-d₄ is the deuterium labeled Clofibrate. Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.

Flurbiprofen axetil solution is mainly composed of Flurbiprofen axetil (HY-101481). Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.