lipolysis

Dehydrocholate sodium, a hydrocholeretic, can increase bile output to clear increased bile acid load.

Acipimox (K-9321) is a niacin derivative and nicotinic acid analog with activity as a hypolipidemic agent. Acipimox has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients.

LEI110 is a potent Phospholipase A2, group XVI (PLA2G16) inhibitor with an Ki value of 20 nM. LEI110 is a selective pan-inhibitor of the HRASLS family of thiol hydrolases (i.e., PLA2G16, HRASLS2, RARRES3 and iNAT).

Glymidine sodium is a sulfonamide hypoglycemic agent which stimulates insulin secretion.

CL316243 is a highly potent selective agonist of β3-adrenoceptor, with a EC50 of 3 nM. CL316243 is an effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.

Gelucire 44/14 (Gelucire 14/44) acts as a nonionic surface-active excipient and improves fat absorption in rats with impaired lipolysis.

Rhododendrol (Frambinol) is a melanin synthesis and acts by preventing high-fat diet-induced elevation in body weight and increasing lipolysis in white adipocytes in male mice. Rhododendrol can be used as the lightening/whitening cosmetics inhibitor.

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

Atglistatin is a highly effective, specific and competitive ATGL inhibitor with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, and no toxicity when the concentration up to 50 μM.

SR-4995 (CID 16016685) is a highly efficient and selective ABHD5 ligand that directly binds to ABHD5 and induces lipolysis by releasing it from PLIN, activating HSL and PLIN1 through PKA-dependent phosphorylation.

Compound 4 (Anti-obesity agent 1) demonstrates potential for enhanced lipolysis, highlighting its anti-obesity characteristics.

Fentomycin is a dual-functional lipolysis-targeting chimera (LIPTAC). It specifically targets plasma membrane phospholipids and, following endocytosis, activates lysosomal iron, which promotes phospholipid oxidation and degradation leading to ferroptosis. This compound effectively kills primary sarcoma and pancreatic ductal adenocarcinoma cells, particularly those subpopulations that are metastatic, drug-resistant, and exhibit high CD44 expression. Fentomycin shows antitumor activity.

C108297 is a glucocorticoid receptor modulator. C108297 prevents both diet-induced obesity and inflammation. C108297 decreased food and fructose intake and increased lipolysis in white adipose tissue (WAT) and free fatty acid levels in plasma, resulting i

E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr

Thermopsoside is a flavonoid derivative isolated from Aspalathus linearis.Thermopsoside inhibits CYP450 isozymes, with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM, and 32.0 μM against CYP3A4, CYP2C19, CYP2D6, and CYP2C9, respectively.

Sinensetin (Pedalitin permethyl ether) is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis.

TRβ agonist 3 (Compound 3) is a potent TRβ agonist and a potential TRβ-selective thyromimetic. In vitro studies show that TRβ agonist 3 reduces lipid accumulation in HepG2 cells and promotes lipolysis [1].

TRβ agonist 2 (Compound 1) is a highly potent TRβ agonist that effectively reduces lipid accumulation in HepG2 cells and promotes lipolysis, offering comparable effects. With its promising attributes, TRβ agonist 2 emerges as a potential thyromimetic selectively targeting TRβ [1].

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.

Acipimox (K-9321) sodium, a nicotinic acid analogue, functions as an antilipolytic agent by stimulating leptin release, inhibiting lipolysis, and reducing systemic free fatty acids (FFAs) levels, thereby enhancing insulin sensitivity.

NG-497 is a selective, small molecule inhibitor of human adipose triglyceride lipase (ATGL) that targets the enzymatically active patatin-like structural domain of human ATGL.NG-497 binds ATGL in a hydrophobic lumen adjacent to the active site.NG-497 abrogates lipolysis in human adipocytes in a dose-dependent and reversible manner.NG-497 has been shown to be useful in cancer research. can be used in cancer research.

Lys-γ3-MSH(human) TFA, a melanocortin peptide originating from the C-terminal fragment of pro-opiomelanocortin (POMC), enhances the steroidogenic response of rat adrenal glands to adrenocorticotrophin (ACTH). It is a potent stimulator of lipolysis, demonstrating an apparent EC50 of 3.56 nM, by activating hormone-sensitive lipase (HSL) and Perilipin A, leading to lipolysis [1] [2].

Z16078526 enhances thermogenesis in mice by inducing endogenous Ucp1 expression, promoting p38 MAPK phosphorylation, and stimulating lipolysis in primary mouse brown adipocytes. Additionally, it activates thermogenic gene expression and mitochondrial activity, specifically uncoupled respiration, in these cells.

Foenumoside B, a triterpene saponin extracted from Lysimachia foenum-graecum, stimulates AMPK signaling, suppresses PPARγ-induced adipogenesis, and promotes lipolysis, shifting lipid metabolism. This compound is utilized in researching obesity and associated metabolic disorders [1].