lipase

Lipase, triacylglycerol (Alkaline lipase) is a specific enzyme that plays an important role in the catabolism of triacylglycerol to glycerol and fatty acids and is required for the transfer of fatty acids to various tissues of the body, and whose transcriptional receipt of transcripts is subjected to nutrient hormonal regulation and is capable of being upregulated by PPARγ,TNFα downregulation, and insulin-mediated downregulation of FOXO1 nuclear localization.

Endothelial lipase inhibitor-1 is a potent inhibitor of endothelial lipase with an IC50 of 49 nM.

Atractylodin (Atractydin) has high lipase inhibitory activity (IC5:39.12 μM); Atractylodin possesses strong repellency activities against T. castaneum adults (LD50: 1.83 μg cm). The repellency of Atractylodin (0.63 μg cm) can achieve >90%.

Lipase Substrate is a compound used to detect lipase activity (substrate).

Monoacylglycerol lipase inhibitor 1, also known as compound 13 [1], is a potent inhibitor of monoacylglycerol lipase.

Pancreatic lipase Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) with an IC50 of 2.13 μM and human carboxylesterase 1A (hCES1A) with an IC50 of 0.055 μM.

Lipoprotein lipase (LPL) is an enzyme, mainly involved in lipid metabolism, that hydrolyzes triglycerides in lipoproteins.LPL can be a target for obesity diabetes-related cardiovascular diseases and has an important role in lowering triglyceride levels and improving cardiovascular.

Monoglyceridelipase is a crucial enzyme involved in lipid metabolism, catalyzing the hydrolysis of monoglycerides (especially 2-AG, or 2-arachidonoylglycerol) into glycerol and free fatty acids. By regulating the levels of 2-AG, this enzyme impacts neural signaling, pain perception, inflammatory responses, and metabolic processes.

Phospholipase D (PLD), an enzyme within the phospholipase superfamily, is prevalent across bacteria, yeast, plants, animals, and viruses, serving roles in biochemical research. It catalyzes the hydrolysis of glycerophospholipids' phosphodiester bonds, generating phosphatidic acid and soluble choline. PLD is implicated in numerous disease-related pathways, such as diabetes, atherogenesis, obesity, tumorigenesis, immune responses, and neuroendocrine functions [1].

Phospholipase A2 (PLA2) is an enzyme that hydrolyzes fatty acids present in the sn-2 position of phospholipids, and is closely related to lipid metabolism and immune function.

1,3-Capryloyl-2-oleoylglycerol is a triglyceride with esterification at specific hydroxyl positions. In this compound, the hydroxyl groups on the 1 and 3 positions of glycerol are acylated with caprylic acid, while the hydroxyl group at the 2 position is acylated with oleic acid.

Beta-Sitosterol (SKF 14463) has recently been shown to induce G2 M arrest, endoreduplication, and apoptosis through the Bcl-2 and PI3K Akt signaling pathways. Beta-Sitosterol (SKF 14463) , a main dietary phytosterol found in plants, may have the potential for prevention and therapy for human cancer. Although the exact mechanism of action of Beta-Sitosterol (SKF 14463) is unknown, it may be related to cholesterol metabolism or anti-inflammatory effects (via interference with prostaglandin metabolism). Beta-Sitosterol (SKF 14463) induces apoptosis and activates key caspases in MDA-MB-231 human breast cancer cells.

JJKK 048 is a potent and selective MAGL inhibitor.

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.

JZP-430 is an effective, highly selective, irreversible inhibitor of α β-hydrolase domain 6 (ABHD6) (IC50: 44 nM). It also shows ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

JNJ-42226314 is a highly selective non-covalent monoacylglycerol lipase (MAGL) inhibitor with anti-injury effects.JNJ-42226314 shows efficacy via endogenous cannabinoid-2-acryloylglycerol (2-AG) in models of neuropathic pain and inflammatory pain.

MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.

JW 642 is an effective inhibitor of monoacylglycerol lipase (MAGL) (IC50: 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively).

WWL70 is a selective inhibitor of alpha beta hydrolase domain 6 with an IC50 of 70 nM.

XEN445, a potent and selective endothelial lipase(EL) inhibitor (IC50=0.237 uM), exhibitis good ADME and PK properties.

JZL195 is a selective and efficacious dual FAAH MAGL inhibitor.

NF-1819 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. NF-1819 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. NF-1819 displays high membrane permeability and brain penetrant.

URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human mouse rat MAGL (IC50: 5.9 15 43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).