PPARα Activator

(10E,12Z)-Octadeca-10,12-dienoic acid (trans-10,cis-12 CLA2) is an orally active PPARα activator and inhibits adipocyte differentiation. (10E,12Z)-Octadeca-10,12-dienoic acid and its downstream metabolites have various antioxidant and antitumor activities. (10E,12Z)-Octadeca-10,12-dienoic acid can induce proinflammatory cytokines and chemokines, which would lead to decreased adipogenesis and insulin resistance in adipose tissue. (10E,12Z)-Octadeca-10,12-dienoic acid can affect many aspects of milk fat synthesis. (10E,12Z)-Octadeca-10,12-dienoic acid reduces expression of lipogenic enzymes and inhibits the desaturation of fatty acids. (10E,12Z)-Octadeca-10,12-dienoic acid can reduce lipoprotein lipase (LPL) activity in cultured 3T3-L1 adipocytes and enhance triacylglycerol release from these cells. (10E,12Z)-Octadeca-10,12-dienoic acid decreases the expression of hepatic stearoyl-CoA desatyrase mRNA in mice. (10E,12Z)-Octadeca-10,12-dienoic acid is associated with changes in mucosal NF-κB and Cyclin D1 protein levels in mice.

Dehydroepiandrosterone sulfate sodium salt-d₆ (DHEA sulfate sodium salt-d₆; Prasterone sulfate sodium salt-d₆) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.

Icariin (Standard) is the analytical standard of Icariin. This product is intended for research and analytical applications. Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC₅₀s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

CUDA 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 selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.

Gemfibrozil (Standard) is the analytical standard of Gemfibrozil. This product is intended for research and analytical applications. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with K_i values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.

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.

AM9053 is a selective, effective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) (IC₅₀ = 30 nM). The effect of AM9053 on FAAH activity is limited (IC₅₀ > 100 nM). AM9053 inhibits the proliferation of colorectal cancer cells by activating the PPAR-α and TRPV1 dependent mechanisms and induces S-phase cell cycle arrest. AM9053 alleviates intestinal fibrosis by regulating macrophage activity and inhibiting the IL-23 signaling pathway. AM9053 leads to an increase in NAE levels, especially PEA and OEA. AM9053 can be used for the study of colorectal cancer and intestinal fibrosis.

Dehydroepiandrosterone sulfate sodium dihydrate-d₆ sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.

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.

13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice.

9(S)-HOTrE is a PPARα activator and an inducer of apolipoprotein A-I (apoA-I) mRNA expression. 9(S)-HOTrE upregulates the expression of PPARα target gene CPT1α. 9(S)-HOTrE can be used in the research of cardiovascular diseases.

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.

Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.

(E)-Osmundacetone (Standard) is the analytical standard of (E)-Osmundacetone (HY-N1966). This product is intended for research and analytical applications. (E)-Osmundacetone is an inhibitor of the MAPK pathway. (E)-Osmundacetone inhibits the activation of the MAPK signaling pathway and restores the expression of PPARα/ACOX1. (E)-Osmundacetone abrogates abnormal cell proliferation, migration and liver metastasis induced by PTPRO silencing in colorectal cancer cells. (E)-Osmundacetone blocks OA-RD17-mediated activation of the MAPK signaling pathway, thereby reducing macrophage proliferation and migration. (E)-Osmundacetone is applicable to relevant research on colorectal cancer.

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.

Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.

Sodium acetate trihydrate, United States Pharmacopeia (USP) Reference Standard (Sodium acetate trihydrate (Pharmaceutical primary standard, USP)) is a carboxylic acid and short-chain fatty acid (SCFAs). Sodium acetate trihydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Sodium acetate trihydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Sodium acetate trihydrate regulates energy metabolism. Sodium acetate trihydrate has anticancer activity against gastric cancer. Sodium acetate trihydrate induces writhing reaction and ulcerative colitis. Sodium acetate trihydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.

GW409544 is a potent PPARα and PPARγ activator, with EC₅₀ values of 2.3 nM and 0.28 nM for PPARα and PPARγ, respectively. GW409544 can be used for the research of metabolic and cardiovascular diseases.

Peroxisome proliferator-activated receptors (PPARs) play an important role in regulating lipid and glucose metabolism, and oleoylethanolamide (OEA) is a natural ligand for PPARα. N-Octadecyl-N'-propyl-sulfamide is an analog of OEA and a potent activator of PPARα, with selective binding affinity for PPARα (EC50=100 nM, compared to 120 nM for OEA). N-Octadecyl-N'-propyl-sulfamide (10 mg/kg; ip) inhibits food intake and reduces body weight gain in rats. At a dose of 1 mg/kg, N-Octadecyl-N'-propyl-sulfamide induces satiety, thereby reducing food intake, body weight, and plasma triglyceride concentrations in free-feeding Wistar rats and obese Zucker (fa/fa) rats.