lipase

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

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

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.

JJKK 048 is a potent and selective MAGL inhibitor.

Cetilistat (ATL-962) is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes.

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).

HSL-IN-1 is an orally active and highly potent hormone-sensitive lipase (HSL) inhibitor that significantly reduces the reactive metabolite load and can reduce the release of free fatty acids from stored fat.

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.

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.

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.

3,4,5-Trihydroxycinnamic acid decyl ester, an effective inhibitor of lipid absorption and accumulation, exhibits anti-obesity properties and acts as a pancreatic lipase inhibitor, with an EC50 of approximately 0.9 μM.

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).

Lalistat 2 is a selective inhibitor of lysosomal acid lipase with IC50 of 152 nM and exhibits no inhibition of human pancreatic lipase or bovine milk lipoprotein lipase (up to 10 μM).

ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM).

Euphol, an alcohol tetracyclic triterpene, has a wide range of pharmacological properties and is considered to have anti-inflammatory action.

MJN110 (Cravatt Reagent) is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110(Cravatt Reagent) Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

Ibrolipim (NO-1886) attenuates high glucose-induced endothelial dysfunction in cultured human umbilical vein endothelial cells via PI3K/Akt pathway.

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) inhibites three SHs (ABHD6, ABHD11, and FAAH)

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

HSL-IN-3 (HSL inhibitor 3) is a boronic acid derivative that is an inhibitor of hormone-sensitive lipase(HSL).

MAGL-IN-5 is a non-selective lipase inhibitor.