PPAR Activator

Methyl dehydroabietate is an orally active resin acid. Methyl dehydroabietate disrupts microbial cell walls and exhibits significant antibacterial activity. Methyl dehydroabietate induces the expression of PPARα in the liver and PPARγ in adipose tissue, and promotes adipocyte differentiation. Methyl dehydroabietate improves insulin resistance, reduces TNFα levels, and alleviates adipocyte hypertrophy and hepatic steatosis in obese mice. Methyl dehydroabietate can be used in research related to obesity, insulin resistance and hepatic steatosis.

SP4f is an activator ofPPAR-γ, with the EC₅₀ of 826 nM in HK-2 cells. SP4f reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice.

CUDA disodium is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC₅₀s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA disodium selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA disodium may be valuable for the research of cardiovascular disease.

ISX-3 is a potent anti-adipogenic and pro-osteogenic agent. ISX-3 increases the expression of PPARγ. ISX-3 has the potential for the research of osteopenia and osteoporosis.

AdipoR agonist 1 (Compound 112254) is an agonist for adiponectin receptor (AdipoR), which activates the transcriptional regulators like peroxisome proliferator-activated receptors (PPARs), peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1α), sirtuin 1 (SIRT1), and adenylate-activated protein kinase (AMPK). AdipoR agonist 1 is utilized in preventive doping research.

1-Methyl Adenosine-d3 is the deuterium labeled 1-Methyladenosine. 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis.

Gemfibrozil-d₆ is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

Monoethyl phthalate-d₄ is the deuterium labeled Monoethyl phthalate. Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms.

(10E,12E)-9-Oxo-10,12-octadecadienoic acid (9-oxo-ODA) is a PPARα agonist that can be isolated from the basidiomycete Gomphus floccosus. (10E,12E)-9-Oxo-10,12-octadecadienoic acid enhances fatty acid oxidation through PPARα activation, thereby inhibiting triglyceride accumulation. (10E,12E)-9-Oxo-10,12-octadecadienoic acid also has antifungal (Fungal) activity.

Ophiopogonin D (Standard) is the analytical standard of Ophiopogonin D. This product is intended for research and analytical applications. Ophiopogonin D can be isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D can inhibit isteoclastic differentiation in RAW264.7 cells. Ophiopogonin D has protective effect as an antioxidant in H₂O₂-induced endothelial injury. Ophiopogonin D blocks ERK signaling cascades. Ophiopogonin D alleviates high-fat diet-induced metabolic syndrome and changes the structure of gut microbiota in mice. Ophiopogonin D has been used against inflammatory, metabolic and cardiovascular diseases.

Triphenyl phosphate-d₁₅ is the deuterium labeled Triphenyl phosphate. Triphenyl phosphate is an orally active, blood-brain barrier-permeable aryl organophosphate flame retardant and endocrine disruptor. Triphenyl phosphate disrupts mitochondrial dynamic balance through oxidative stress, induces excessive mitophagy and apoptosis, and ultimately leads to myocardial fibrosis. In the brain, Triphenyl phosphate activates the NF-κB inflammatory pathway by disrupting the gut microbiota, alters tryptophan metabolism and elevates neurotoxins, thereby inducing anxiety- and depression-like behaviors. In the skeletal and reproductive systems, Triphenyl phosphate inhibits osteoblast differentiation and induces germ cell apoptosis by suppressing the MAPK/ERK pathway and activating the JNK signal, respectively. In adipose and placental tissues, Triphenyl phosphate promotes lipid accumulation by activating the PI3K/AKT-PPARγ axis, and disrupts placental metabolism via the MAOA/ROS/NF-κB cascade, impairing neurodevelopment of offspring.

9-HEPE, a oxidation product of Eicosapentaenoic acid, is a racemic mixture of 9(R)-HEPE and 9(S)-HEPE. 9-HEPE induces fatty acid oxidation, adipogenesis, and glucose uptake via activation of PPARs in vivo.

20-Carboxyarachidonic acid, a relatively stable metabolite of 20-HETE, is an endogenous dual activator of PPARalpha and PPARgamma.

Palmitelaidic acid-d₁₃ is the deuterium labeled Palmitelaidic Acid. Palmitelaidic Acid (9-trans-Hexadecenoic acid) is the trans isomer of palmitoleic acid. Palmitoleic acid is one of the most abundant fatty acids in serum and tissue.

SP4e is an activator of PPAR-γ, with the EC₅₀ of 739 nM in HK-2 cells. SP4e reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice.

Pioglitazone-d₄ is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2), a metabolite of PGD2 (HY-101988), is an agonist of prostaglandin receptor 2 (DP2). 15-deoxy-Δ12,14-Prostaglandin D2 binds to DP2 (Ki=50 nM) and induces eosinophil activation (EC₅₀=8 nM). 15-deoxy-Δ12,14-Prostaglandin D2 also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), inducing PPARγ-mediated transcription. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is cytotoxic to L1210 murine leukemia cells (IC₅₀=0.3 μg/ml) and inhibits ADP-induced platelet aggregation (IC₅₀=320 ng/mL).

Daidzein-d₆ is a deuterium labeled Daidzein (HY-N0019). Daidzein is a soy isoflavone, which acts as a PPAR activator.

Pioglitazone-d₄ (alkyl) (U 72107-d₄ (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

Sodium propionate-d₃ is the deuterium labeled Propionate sodium (HY-B1773A). Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.