PPARγ Activator

Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC₅₀: 45 nM), DNA methyltransferases (IC₅₀: 18.6 nM) and aminopeptidase N (APN) (IC₅₀: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis.

Garcinia cambogia extract is an orally active anti-obesity agent. Garcinia cambogia extract upregulates the gene expression of aP2, SREBP1c, PPARγ2 and C/EBPα. Garcinia cambogia extract reduces the rate of body weight gain, visceral fat accumulation, lipid levels in blood and liver, as well as plasma insulin and leptin levels. Garcinia cambogia extract ameliorates high-fat diet-induced obesity.

Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ.

Tartronic acid, a dicarboxylic acid derive, is an inhibitor of the transformation of carbohydrates into fat under fat-deficient diet conditions. Tartronic acid promotes 3T3-L1 adipocyte differentiation by increasing the protein expression of FABP-4, PPARγ and SREBP-1. Tartronic acid promotes de novo lipogenesis and inhibits CPT-1β by upregulating acetyl-CoA and malonyl-CoA. Tartronic acid promotes weight gain and induces adipocyte hypertrophy in epididymal white adipose tissue and lipid accumulation in the livers of high-fat diet induced obese mice. Tartronic acid can be used for lipid metabolic disease research.

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC₅₀ values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y₁₄R (IC₅₀ = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.

Sulindac sulfone is an orally active metabolite of Sulindac (HY-B0008). Sulindac sulfone activates PPARγ and drives transcriptional induction of SSAT by binding to the PPRE-2 element. Sulindac sulfone induces Apoptosis. Sulindac sulfone negatively regulates the function of VDAC1/2 to inhibit the mTORC1 pathway, reduces Cyclin D1 levels, and induces G₁ cell cycle arrest in colon cancer cells. Sulindac sulfone exerts colon cancer preventive effects through a COX-independent mechanism. Sulindac sulfone can be used in research related to colon cancer.

Karacoline is an orally active PPARγ activator and ERK/JNK MAPK inhibitor. Karacoline restricts ROS production, maintains mitochondrial membrane potential, and inhibits pulmonary cell apoptosis. Karacoline inhibits NF-κB pathway activation, reduces acetylation levels of p65 and the expression of MMP14 and MMP9, enhances the expression of type II collagen (collagen II) and aggrecan (aggrecan), and suppresses extracellular matrix degradation. In a mouse model of sepsis-induced acute lung injury, Karacoline alleviates lung injury, inhibits the release of IL-1β, IL-6 and TNF-α, increases the Bcl-2/BAX ratio, and reduces caspase 3 expression. Karacoline can be used in research related to acute lung injury and intervertebral disc degeneration.

Glabridin (Standard) is the analytical standard of Glabridin. This product is intended for research and analytical applications. Glabridin is a natural isoflavan from Glycyrrhiza uralensis, binds to and activates PPARγ, with an EC₅₀ of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.

9 (10)-Nitrooleate (9(10)-Nitrated oleic acid) is an endogenous lipid signaling mediator with vasoprotective effects. 9 (10)-Nitrooleate enhances enzymatic activity and improves nitric oxide bioavailability by inducing phosphorylation of Akt and ERK1/2, regulating the multi-site phosphorylation status of eNOS and optimizing its interaction with Hsp90. 9 (10)-Nitrooleate also activates PPARα, PPARδ and PPARγ receptors, thereby regulating adipogenesis, glucose uptake and inflammation-related gene expression, and exhibits immunosuppressive effects by inhibiting neutrophil migration and cytokine secretion. 9 (10)-Nitrooleate is widely used in studies of sepsis and related inflammatory diseases.

Adelmidrol exerts important anti-inflammatory effects that are partly dependent on PPARγ. Adelmidrol reduces NF-κB translocation, and COX-2 expression.

MMPP is an orally active inhibitor of STAT3 and VEGFR2, as well as an activator of PPARγ. MMPP blocks the VEGFR2/AKT/ERK/NF-κB signaling pathway to inhibit angiogenesis. MMPP inhibits ferroptosis and inflammation, and alleviates sepsis-induced myocardial injury. MMPP induces G1-phase cell cycle arrest and apoptosis, and inhibits the growth of non-small cell lung cancer (NSCLC) and solid tumors. MMPP promotes adipogenesis and glucose uptake. MMPP can be used in research related to NSCLC, type 2 diabetes and myocardial injury.

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC₅₀ = 3.4 μM) and 5-lipoxygenase (5-LOX; IC₅₀ = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (K_D = 10-14 μM). YS121 dose-dependently reduces PGE₂ production with an EC₅₀ of 12 μM in IL-1β-stimulated A549 cells. YS121 (compound 9) activates PPAR-α and -γ (EC₅₀ = 1 and 3.6 μM, respectively). YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research.

Ambrosin is an orally active NF-κβ and BACE1 inhibitor. Ambrosin reduces pro-inflammatory and nitrosative mediators, increases PPARγ levels, inhibits apoptosis (Apoptosis), enhances autophagy (Autophagy), and ameliorates oxidative stress. Ambrosin reduces Amyloid plaque deposition. Ambrosin improves lipopolysaccharide-induced memory impairment and colonic histopathological changes. Ambrosin can be used in research related to Alzheimer's disease and colitis.

NO-Pravastatin is a derivative of Pravastatin (HY-B0165) covalently linked with an NO donor moiety, endowing it with dual functions of HMG-CoA reductase (HMGCR) inhibition and exogenous nitric oxide (NO) release. NO-Pravastatin activates PPARα/γ and ABCA1, and inhibits LPS (HY-D1056)-induced TNFα production. NO-Pravastatin can be used in research related to gallstones and cardiovascular diseases.

HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC₅₀ values of 6.09 nM and 8.06 nM, and K_d values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease.

Apo-12'-lycopenal is a Lycopene (HY-N0287) metabolite. Apo-12'-lycopenal promotes adipocyte differentiation and adiponectin secretion via PPAR-γ activation.

GW9820 is PPARα and PPARγ activator (EC₅₀s: 0.37 μM for PPARα; 0.288 μM for PPARγ). GW9820 increases CLA-1. GW9820 can be used in the research of atherosclerosis.

Zaltoprofen sulfoxide (Compound M2) is the main metabolite of Zaltoprofen (HY-B0619). Zaltoprofen sulfoxide is an efficient and selective COX-2 inhibitor (IC₅₀ = 45.38 nM) and a PPAR-γ activator. Zaltoprofen sulfoxide effectively inhibits NF-κB and MAPK inflammatory signaling pathways and alleviates acute lung injury induced by LPS (HY-D1056B3). Zaltoprofen sulfoxide can be used for the study of acute lung injury.

(Rac)-Pinostrobin ((±)-Pinostrobin) is a dual agonist of TGR5 and PPARγ. (Rac)-Pinostrobin specifically activates TGR5 without acting on other endogenously expressed GPCRs. (Rac)-Pinostrobin exhibits moderate PPARγ activation activity. (Rac)-Pinostrobin possesses metabolic regulatory activity. (Rac)-Pinostrobin can be used in research related to obesity and type 2 diabetes.

15-Keto-prostaglandin E2-d₉ is the d₉ labeled 15-keto-Prostaglandin E2 (HY-113205). 15-keto-Prostaglandin E2 (15-keto-PGE2) is an endogenous PGE₂ metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to the Cys259 residue of STAT3. 15-keto-Prostaglandin E2 binds to and stabilizes EP2 and EP4 receptors. 15-keto-Prostaglandin E2 inhibits the growth and progression of breast cancer cells. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth. 15-keto-Prostaglandin E2 disrupts glomerular vascularization during zebrafish development and reduces the surface area of the glomerular filtration barrier.