PPARγ Modulator

Fmoc-Leucine (N-FMOC-leucine) is an anti-inflammatory agent that not only promotes extracellular Ca²⁺ influx but also facilitates intracellular Ca²⁺ release. Fmoc-Leucine is a selective ligand for PPARγ (K_i = 15 μM), exhibiting insulin-sensitizing effects but with weak fatogenic activity. Fmoc-Leucine exhibits unique self-assembly properties and can form transient gels, stable gels, or crystals/2D sheets through different pathways. Fmoc-Leucine can be used in the research of diabetes, colitis, and bladder cancer.

Azemiglitazone potassium (MSDC-0602K), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC₅₀ of 18.25 μM. Azemiglitazone potassium modulates the mitochondrial pyruvate carrier (MPC). Azemiglitazone potassium can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance. Azemiglitazone potassium, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide.

Perfluoropentanoic acid (PFPeA), a short-chain perfluorinated compound, serves as an important indicator of perfluorinated compound pollution in ecosystems. Perfluoropentanoic acid exhibits certain toxicity to mice.

Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC₅₀ of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus.

ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC₅₀s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC₅₀ s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model.

GED 0507-34-Levo is an orally active PPARγ modulator. GED 0507-34-Levo downregulates the expression of TGF-β, Smad3, IL-13, and CTGF in the colon. GED 0507-34-Levo improves DSS-induced chronic colitis and fibrosis.

PPARγ/δ modulator 2 (Compound 3h) is a PPARγ agonist and PPARδ antagonist. The K_i values for PPARγ and PPARδ are 2.8 μM and 43 nM, respectively. PPARγ/δ modulator 2 significantly enhances the production of Adiponectin and promotes adipogenic differentiation of human bone marrow mesenchymal stem cells (hBM-MSCs). PPARγ/δ modulator 2 can be used in the study of metabolic disorders associated with hypoadiponectinemia.

PA-082 is a selective PPAR-γ modulator that functions as a partial agonist. PA-082 causes partial recruitment of SRC1, TIF2, SRC3 and full recruitment of PGC1-α to PPAR-γ ligand-binding domain. PA-082 prevents triglyceride accumulation during de novo adipogenesis and antagonizes Rosiglitazone (HY-17386)-induced lipid accumulation. PA-082 potentiates insulin-stimulated glucose uptake in adipocytes and protects against TNFα-induced insulin resistance. PA-082 can be used for the research of type 2 diabetes.

PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with K_i values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC₅₀ of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively.

SR2595 is an inverse agonist of PPARγ with an IC₅₀ of 30 nM.

Anticancer agent 183 (example 48) is a non-agonistic PPARG modulator. Anticancer agent 183 has a high affinity to PPARG (PPARγ). Anticancer agent 183 inhibits kinase-mediated phosphorylation of PPARG. Anticancer agent 183 can used for research on metabolic diseases to avoid side effects.

PPARγ modulator-3 (Compound 11) is a peroxisome proliferator-activated receptor γ (PPARγ) modulator with a K_D value of 186 nM. PPARγ modulator-3 is promising for research of insulin resistance (IR)-related diseases, such as type 2 diabetes mellitus (T2DM) and metabolic syndrome.

YGT-31 is a modulator for PPARγ with an IC₅₀ of 1.72 μM, and a K_i of 0.62 μM. YGT-31 reduces blood glucose levels and improves insulin resistance in db/db mice type 2 diabetes models, through inhibition of CDK5-mediated PPARγ-Ser273 phosphorylation. YGT-31 exhibits anti-hepatic steatosis effect in mice non-alcoholic fatty liver disease (NAFLD) model.

PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC₅₀ of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models.