PPAR Agonist

L-165041 is a cell permeable PPARδ agonist, with K_is of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.

Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.

Ciprofibrate (Win35833) is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate acts as an orally active hypolipidaemic agent and can be used for the research of primary hyperlipidaemias.

10-Hydroxystearic acid (10-HSA) is a PPARα agonist. 10-Hydroxystearic acid stimulates collagen synthesis. 10-Hydroxystearic acid is an anti-aging agent and reduces the appearance of pores and hyperpigmented lesions.

Retinoic acid-d₅ is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC₅₀s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with K_d of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.

Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice.

SC-236 is an orally active COX-2 specific inhibitor (IC₅₀ = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model.

Leriglitazone (MIN-102; Hydroxypioglitazone) is an orally active and a BBB-penetrable PPARγ agonist with an EC₅₀ of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases.

Raspberry ketone is a major aromatic compound of red raspberry, widely used as a fragrance in cosmetics and as a flavoring agent in foodstuff; also shows PPAR-α agonistic activity.

25-Hydroxytachysterol3 is the metabolite of Vitamin D3 (HY-15398). 25-Hydroxytachysterol3 inhibits the proliferation of epidermal keratinocytes and dermal fibroblasts, stimulates the expression of differentiation- and antioxidant-related genes in keratinocytes. 25-Hydroxytachysterol3 activates vitamin D receptor (VDR) and aryl hydrocarbon receptor (AhR), liver X receptor α/β (LXR α/β) and peroxisome proliferator-activated receptor γ (PPARγ), stimulates the expression of CYP24A1.

Balaglitazone is a selective partial PPARγ agonist with an EC₅₀ of 1.351 μM for human PPARγ.

Saroglitazar magnesium 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.

Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride is an orally active and a BBB-penetrable PPARγ agonist with an EC₅₀ of 9 μM. Leriglitazone hydrochloride, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone hydrochloride can be used in the study of neuroinflammatory and neurodegenerative diseases.

PPARα/γ agonist 1 (compound 5b) is a potent and dual PPARα/γ partial agonist with EC₅₀ values of 28 nM and 69 nM for PPARα and PPARγ, respectively. PPARα/γ agonist 1 is a promising prototype for dyslipidemia and diabetes research.

Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC₅₀ of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC₅₀ of ~1 μM for PPARα/PPARβ.

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

Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.

Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.

Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC₅₀s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity.

ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ.