PPAR Agonist

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.

Rosiglitazone (maleate) (Standard) is the analytical standard of Rosiglitazone (maleate). This product is intended for research and analytical applications. Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

Pparδ agonist 1 is a PPAR-δ agonist, with an EC₅₀ of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.

Mavodelpar free acid is a PPARδ agonist extracted from patent US20180071304, compound example 10. Mavodelpar (free acid) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Sodelglitazar (GW 677954) is a pan-PPAR agonist with potential applications in the treatment of hyperlipidemia and type 2 diabetes.

Isobutylparaben-d₄ is the deuterium labeled Isobutylparaben. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.

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.

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.

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.

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.

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.

ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research.

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

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.

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.

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.

Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.

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.

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.