PPAR Agonist

Perfluoro (2-methyl-3-oxahexanoic) acid (HFPO-DA) is an orally active PPARα agonist with an EC₅₀ of 2.1 μM for human PPARα. Perfluoro (2-methyl-3-oxahexanoic) acid induces peroxisome proliferation and increases the levels of proinflammatory mediators. It impairs intestinal barrier function and disrupts cecal flora balance. Perfluoro (2-methyl-3-oxahexanoic) acid is applicable to research related to developmental toxicity, hepatotoxicity and intestinal toxicity.

Retinoic acid (Vitamin A acid) (GMP) is Retinoic acid (HY-14649) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Retinoic acid is an agonist of RAR nuclear receptors.

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.

Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity..

Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM.

Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC₅₀ values of 0.65 pM and 3 nM in HepG2 cells, respectively.

15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC₅₀ of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC₅₀ of 7 μM.

Tesaglitazar is a dual-target PPARα/γ agonist with an EC₅₀ of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain.

Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone is the orally active agonist for PPAR with EC₅₀ of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.

MTX-531 is an oral drug that inhibits EGFR (with an IC₅₀ of 14.7 nM) and PI3K (with IC₅₀ values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC₅₀ of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors.

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.

Ciglitazone is a potent and selective PPARγ agonist (EC₅₀=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells.

Rosiglitazone (Standard) is the analytical standard of Rosiglitazone. This product is intended for research and analytical applications. Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

AMG131 (INT131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 is promising for research of type-2 diabetes mellitus.