PPARγ Agonist

LCI765 is an orally active and selective PPARδ agonist, with an EC₅₀ of 0.07 nM. LCI765 can be used for the research of diseases related to energy homeostasis such as metabolic syndrome.

PPARγ agonist-21 (Compound 9a) is a PPARγ agonist with an EC₅₀ of 3.12 μM. PPARγ agonist-21 activates PPAR-γ to inhibit NF-κB and attenuate NLRP3 inflammasome assembly. PPARγ agonist-21 blocks NLRP3-ASC and NLRP3-NEK7 interaction. PPARγ agonist-21 attenuates the severity of gouty arthritis.

15-LOX-IN-2 (Compound 2a) is an orally active COX-2/15-LOX inhibitor and a partial agonist of PPARγ. 15-LOX-IN-2 has anti-inflammatory activity and inhibits the levels of 20-HETE, IL-1β and TNF-α in RAW 264.7 cells treated with LPS (HY-D1056). In addition, 15-LOX-IN-2 has significant glucose uptake capacity in the absence of insulin. 15-LOX-IN-2 can be used for the research of metabolic diseases.

GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC₅₀ of 3 μM by using Ba²⁺ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrial membrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells.

DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes.

2'-Hydroxy-4-methoxychalcone is a PPARγ agonist. 2'-Hydroxy-4-methoxychalcone also exhibits inhibitory activity against gelatinase/collagenase and human glutathione S-transferase (GST), with an IC₅₀ of 5.2 μM and a K_i of 15.36 μM against GST. 2'-Hydroxy-4-methoxychalcone inhibits both the NF-κB and AP-1 signaling pathways, exerting anti-inflammatory activity; it also inhibits COX-2, conferring anti-cancer/anti-angiogenic activity. 2'-Hydroxy-4-methoxychalcone can be used in studies related to atherosclerosis, inflammatory diseases and cancer.

PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with K_is of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes.

PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC₅₀ values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent.

PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC₅₀ values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis.

PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC₅₀ values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes.

PPARγ agonist-26 is a PPARγ agonist with an EC₅₀ of 98.43 μM. PPARγ agonist-26 is non-cytotoxic and does not inhibit α-glucosidase. PPARγ agonist-26 induces migration of HEK 293 cells. PPARγ agonist-26 can be used for research on PPAR-γ-related diseases, such as diabetes.

Prostaglandin B₃ (PGB₃) is a member of the class of prostaglandins B and a secondary alcohol. PGB₃ exhibits a rather low affinity to human PPARγ with a K_i value greater than 1 mM compared with K_i values of 26.28 ± 8.7 μM for PGB₁ and 77 ± 37.7 μM for PGB₂.

Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy.

TZD18 is a potent and orally active PPARα and PPARγ dual agonist with IC₅₀ values of 0.028, 0.057, >10 µM for PPARα, PPARγ, PPARδ, respectively. TZD18 reduces plasma levels of both glucose and triglycerides in diabetic mice. TZD18 has the potential for the research of type 2 diabetes.

CLX-0921 is an orally active PPARγ agonist with an IC₅₀ of 1.54 μM. CLX-0921 has a potent antihyperglycemic activity, and can be used for the study of type 2 diabetes.

7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one is a dual agonist of PPARα and PPARγ, with an EC₅₀ of 23.10 μM for human PPARα and an EC₅₀ of 22.29 μM for human PPARγ. 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one regulates the expression of lipid metabolism-related genes via PPARα, and modulates the expression of genes associated with glucose homeostasis and adipogenesis via PPARγ. 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one can be used in the research of type 2 diabetes and metabolic syndrome.

NS-220 is an orally active PPARα agonist with high subtype selectivity, with EC₅₀ values of 1.9×10^-8 M, 9.6×10^-6 M and >10^-4 M for PPARα, PPAR γ and PPARδ, respectively. NS-220 is used in the research for hyperlipidemia or metabolic disorders in type-2 diabetes.