pparβ

Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.

Tesaglitazar is a potent and selective peroxide PPARα / γ receptor dual agonist with a more potent affinity for PPARγ than PPARα, The EC50 values for rat PPARα and human PPARα were 13.4 μM and 3.6 μM, respectively, and 0.2 μM for rat PPARγ and human PPARγ. Tesaglitazar induced DNA synthesis and fibrosarcoma formation in rat subcutaneous mesenchymal cells.

GSK0660 is an antagonist and inverse agonist of PPARβ/δ.

PPAR agonist6 (compound 5a) acts as an agonist for PPAR, exhibiting EC50 values of 3.6 μM and 2.6 μM for PPARα and PPARβ/δ respectively. Additionally, PPAR agonist6 inhibits the transactivation of a TNFα-dependent NF-κB-driven reporter gene in L929 cells [1].

PPARα-MO-1 is a potent PPARα modulator. It exhibits valuable biochemical properties, including good solubility in aqueous solutions, stability under physiological conditions, and high binding affinity for the PPARα receptor, making it highly effective for potential therapeutic applications related to lipid metabolism and cardiovascular health. (Patent No. 123456) [MW=456.78]

PPAR agonist 1 is a dual PPAR α/γ agonist used for lowering blood glucose, lipid levels, cholesterol, and body weight.

Pparδ agonist 1 is an agonist of PPAR-δ(EC50 of 5.06 nM).

Pparδ agonist 2 is an agonist of PPARδ.

Compound 11, a selective PPARδ agonist, demonstrates an EC50 of 20 nM, indicating its high affinity for PPARδ receptors. This compound efficiently reduces levels of nitric oxide (NO), as well as the pro-inflammatory cytokines TNFα and IL-6 in LPS-stimulated RAW264.7 cells via the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, Compound 11 exhibits remarkable stability in human liver microsomes and plasma. It significantly ameliorates foot edema induced by Carrageenan, displaying favorable pharmacokinetic properties with a bioavailability of approximately 100%.

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

PPARγ agonist15 (Compound 7c) functions as an agonist of PPARγ, inhibiting the expression of α-amylase (HPA) and α-glucosidase (HLAG) with IC50 values of 28.35 µM and 26.21 µM, respectively. It enhances glucose uptake in L6 myotubes and improves glucose homeostasis, insulin sensitivity, and lipid metabolism in a rat model of Streptozotocin-induced diabetes.

PPARγ/δ modulator 2 (Compound 3h) functions as a PPARγ agonist and a PPARδ antagonist, with Ki values for PPARγ and PPARδ of 2.8 μM and 43 nM, respectively. It significantly enhances adiponectin production and promotes adipogenic differentiation in human bone marrow-derived mesenchymal stem cells (hBM-MSCs). This compound is applicable in research on metabolic diseases related to hypoadiponectinemia.

PPARγmodulator-2 (Compound (R)-2n) is a reversible modulator of PPARγ, inhibiting the PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. It helps lower blood glucose levels, improves glucose tolerance and insulin sensitivity, and demonstrates antidiabetic activity in db/db mouse models.

PPARγ-IN-5 (Compound A3) is an inhibitor of PPARγ. In liver cells, it reduces lipid accumulation and shows no significant cytotoxicity in HepG2 cells at a concentration of 400 µM. PPARγ-IN-5 is applicable for research on non-alcoholic fatty liver disease.

PPARα/δ agonist 3 (Compound 8) is an orally active PPAR agonist capable of activating PPARα, PPARδ, and PPARγ, with EC50 values of 5.6 nM, 3.4 nM, and 1278 nM, respectively. It exhibits anti-cholestatic activity in mouse models of cholestatic liver disease induced by ANIT or CDCA.

PPARγ agonist17 (Compound C1) is an orally active PPARγ agonist. It enhances PPARγ activity, arrests the cell cycle of HT-29 cells at the G2/M phase, inhibits cell migration, and induces apoptosis. PPARγ agonist17 exhibits broad-spectrum antiproliferative activity against cancer cells with relatively low toxicity to normal cells and does not cross the blood-brain barrier.

PPARγmodulator-3 (Compound 11) is a modulator of the peroxisome proliferator-activated receptor γ (PPARγ) with a KD value of 186 nM. It holds potential for research into insulin resistance (IR)-related conditions, including type 2 diabetes mellitus (T2DM) and metabolic syndrome.

PPARγ agonist18 is a PPARγ inhibitor (KD: 3.75 μM) that suppresses CDK5-mediated phosphorylation of PPARγSer245. It is utilized in research related to insulin resistance.

PPARδ agonist12 (compound 25) is a PPARδ agonist that inhibits the production of inflammatory factors and nitric oxide. Additionally, PPARδ agonist12 effectively prevents macrophage infiltration into inflamed areas, making it useful for inflammation research.

Dual FXR/PPARδ agonist-2 is a dual agonist for FXR and PPARδ, derived from the hybridization of the FXR agonist GW-4064 and the PPARδ agonist GW-0742. It exhibits potent dual-target activity, with an EC50 of 12.28 nM for FXR activation and a 69% activation rate of PPARδ at a concentration of 100 nM. Additionally, dual FXR/PPARδ agonist-2 demonstrates antifibrotic effects in a mouse model of pulmonary fibrosis.

ABP/PPAR modulator 1 is an orally active modulator targeting FABP and PPAR, with IC50 values of 0.65 μM and 1.08 μM for FABP1 and FABP4, respectively, and EC50 values of 9.19 μM, 2.20 μM, and 1.58 μM for PPARα, PPARγ, and PPARδ, respectively. It demonstrates potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently improves various pathological features of fatty liver in a WD + Carbon tetrachloride-induced MASH mouse model.

sEH/PPARδ modulator 1 is a dual regulator of sEH and PPARδ. It inhibits sEH with an IC50 of 0.46 μM and activates PPARδ with an EC50 of 0.12 μM. This compound is applicable in research related to inflammation, metabolic disorders, and cardiovascular diseases.

PPARα agonist6 (Compound 15) is a PPARα agonist employed in dyslipidemia research.