Lipase Inhibitor

Fucoxanthinol, a carotenoid, is a deacetylated Fucoxanthin (HY-N2302) metabolite with oral activity, and inhibits rat pancreatic lipase with an IC₅₀ of 764 nM. Fucoxanthinol reduces expression of Bcl-2, Bcl-xL, survivin, XIAP, cIAP2, cyclin D1, cyclin D2, cyclin E, CDK4, CDK6, β-catenin, JunD, PPARγ, and induces GADD45α expression. Fucoxanthinol activates caspase-3, caspase-8, caspase-9, Nrf2/Keap1/ARE pathway, and inhibits activation of Akt, NF-κB, AP-1, PDPK1, GSK3β phosphorylation. Fucoxanthinol induces apoptosis, G0/G1 cell cycle arrest, inhibits cancer cell viability, proliferation, migration, invasiveness, tumour growth, adipocyte differentiation, oxidative stress, neurotoxicity, triglyceride absorption, angiogenesis, and obesity-induced inflammation. Fucoxanthinol can be used for the research of osteosarcoma, leukemia, lymphoma, adult T-cell leukemia, prostate cancer, colon cancer, breast cancer, hypertriglyceridaemia, Alzheimer’s disease, Parkinson’s disease, obesity, insulin resistance, malignant melanoma, and type II diabetes.

Vulgarin is an orally active, naturally occurring eudesmane sesquiterpene with multiple biological activities including anti-inflammatory and antioxidant properties. Vulgarin targets and inhibits HMGB1, NF-κB and iNOS, while regulating key genes involved in hepatic gluconeogenesis; it also blocks inflammatory signaling pathways and inhibits the production and release of pro-inflammatory cytokines such as TNF-α and IL-1β. Vulgarin effectively alleviates pancreatic oxidative stress by reducing lipid peroxidation levels and restoring antioxidant enzyme activity. Vulgarin reverses abnormally elevated serum pancreatic enzyme levels, preserves the integrity of pancreatic acinar cells, and reduces pancreatic edema, hemorrhage and inflammatory infiltration. Vulgarin remodels the function of pancreatic endocrine cells, restores insulin content in β cells, and downregulates glucagon levels in α cells and somatostatin levels in δ cells. Vulgarin can be used in studies related to pancreatic injury and diabetes.

Aspulvinone H is an orally active inhibitor of AChE, pancreatic lipase, glutamic-oxaloacetic transaminase 1, and α-glucosidase, with IC₅₀ values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It has a K_a of 2.14 μM against GOT1 and a K_i of 6.58 μM against α-glucosidase. Aspulvinone H inhibits cancer cell proliferation, interferes with glutamine metabolism, elevates ROS levels, and induces cell apoptosis and S-phase arrest. Aspulvinone H exhibits antibacterial activity against Staphylococcus aureus. Aspulvinone H inhibits the growth of pancreatic ductal adenocarcinoma xenografts. Aspulvinone H reduces postprandial blood glucose in mice. Aspulvinone H can be used in research related to pancreatic ductal adenocarcinoma, diabetes, and Staphylococcus aureus infection.

4'-O-Methylcatechin acts as a lipase and acetylcholinesterase inhibitor, with an IC₅₀ of 149.93 μM against lipase and an IC₅₀ of 230.89 μM against electric eel-derived acetylcholinesterase. 4'-O-Methylcatechin possesses free radical scavenging activity and can be used in studies on antioxidation, antilipase activity and dementia.

Glucovanillin, found in vanilla, is a potential lipase inhibitor. Glucovanillin can be converted into vanillin through an enzyme-coupled process involving cell wall degradation and glucovanillin hydrolysis.

Ligupurpuroside A is an active product that can be extracted from Ligustrum robustum. Ligupurpuroside A acts as a natural inhibitor of lipase in a competitive manner.

Panclicin A is a potent pancreatic lipase inhibitor.

Panclicin C is a potent pancreatic lipase inhibitor.

Escin IB (Standard) is the analytical standard of Escin IB. This product is intended for research and analytical applications. Escin IB is a saponin isolated from skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum). Escin IB shows inhibitory effect on pancreatic lipase activity.

Panclicin E is a potent pancreatic lipase inhibitor.

hPL-IN-1 (compound 2t) is a reversible inhibitor of pancreatic lipase (PL) (IC₅₀=1.86 μM) for anti-obesity research.

BAY 59-9435 (Standard) is the analytical standard of BAY 59-9435 (HY-102056). This product is intended for research and analytical applications. BAY 59-9435 is a potent and selective inhibitor of Hormone Sensitive Lipase (HSL), with an IC₅₀ of 0.023 μM.

Panclicin D is a potent pancreatic lipase inhibitor.

DO53 is a serine hydrolase inhibitor that targets ABHD6, PAFAH2, PLA2G7, ABHD2 and CES1C. DO53 reduces LPS (HY-D1056A1)-induced cytokine production in the mouse brain, decreases fasting-induced refeeding behavior, and induces hypoactivity in mice. As a DAGL negative control, DO53 shows no activity against DAGLα/β in vivo, and does not affect brain lipid levels, DSE/DSI synaptic plasticity or LPS-induced anhidrosis in mice. DO53 can be used in studies related to LPS-induced neuroinflammation and fasting-induced refeeding.

Gluconapin (3-Butenyl glucosinolate) is an orally active aliphatic glucosinolate and also a flavor modifier. Gluconapin inhibits the elevation of plasma triglyceride levels in mice. Gluconapin also exhibits certain antibacterial activity.

Panclicin B is a potent pancreatic lipase inhibitor.

HSL-IN-1 (Standard) is the analytical standard of HSL-IN-1 (HY-101509). This product is intended for research and analytical applications. HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC50=2 nM) with a significantly reduced reactive metabolite liability.

Pancreatic lipase-IN-1 (compound 8) ia a pancreatic lipase inhibitor with the K_i of 1.288 μM.