Lipase Inhibitor

Royleanonic acid is an abietan-type diterpene found in the leaves of Salvia officinalis L. Royleanonic acid is a porcine pancreatic lipase inhibitor with an IC₅₀ of 35 μg/mL.

Pungenin is a compound that can be isolated from Leontopodium leontopodioides. Pungenin exhibits lipase inhibitory activity. Pungenin reuduces triglyceride absorption.

Hi 76-0079 (NNC0076-0079; 76-0079) is a lipase inhibitor that specifically targets hormone-sensitive lipase (HSL). Hi 76-0079 inhibits PNPB Hydrolysis in cell lysates of HEK293A cells overexpressing Lipe with an IC₅₀ value of 0.1 μM. Hi 76-0079 synergizes with the ATGL inhibitor Atglistatin (HY-15859) to block lipolysis in vitro. Hi 76-0079 can be used for the study of lipid metabolism.

BAY 59-9435 is a potent and selective inhibitor of Hormone Sensitive Lipase (HSL), with an IC₅₀ of 0.023 μM.

Dehydrocholic acid (Dehydrocholate) is an orally active hydrocholeretic agent. Dehydrocholic acid modulates Autophagy, reduces serum amylase and lipase levels. Dehydrocholic acid has the effects of promoting choleretic function, protecting the liver, reducing pancreatic damage, and regulating cholesterol metabolism. Dehydrocholic acid can be used in the study of acute biliary pancreatitis and obstructive jaundice.

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.

XEN445 is a potent, selective and orally active endothelial lipase (EL) inhibitor with an IC₅₀ value of 0.237 μM. XEN445 selectively inhibits phospholipase enzymatic activity of LIPG. XEN445 raises plasma HDL and cholesterol levles. XEN445 induces G1 cell cycle arrest, reduces cell viability, suppresses cancer stem cell self-renewal, and inhibits tumor formation in LIPG-expressing triple-negative breast cancer cells, while showing no inhibitory effect on invasiveness or cancer stem cell stemness in these cells. XEN445 can be used for the research of cancer and metabolic disease, such as triple-negative breast cancer.

GSK264220A is a potent endothelial lipase inhibitor with IC₅₀ of 16 nM. GSK264220A has the potential to decrease the risk of cardiovascular disease.

Isorhamnetin-3-O-glucoside is an orally active natural compound. Isorhamnetin 3-O-glucoside increases P-ERK, ERK, P-Akt (Ser473), P-PI3K, and PDX-1. Isorhamnetin 3-O-glucoside downregulates C/EBPα and inhibits lipase. Isorhamnetin 3-O-glucoside reduces lipids and inhibits obesity.

Dehydrocholic acid (Dehydrocholate) sodium is an orally active hydrocholeretic agent. Dehydrocholic acid sodium modulates Autophagy, reduces serum amylase and lipase levels. Dehydrocholic acid sodium has the effects of promoting choleretic function, protecting the liver, reducing pancreatic damage, and regulating cholesterol metabolism. Dehydrocholic acid sodium can be used in the study of acute biliary pancreatitis and obstructive jaundice.

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.

Rhodionin is an orally active, multifunctional antivirulence and cytoprotective agent that targets and inhibits Lipase, sortase A (SrtA), CYP2D6 (IC₅₀=0.761 μM), AChE (IC₅₀=2.43-57.5 μM), and DPPH free radicals (IC₅₀=19.49 μM). Rhodionin is isolable from the roots of Rhodiola crenulata. Rhodionin reduces postprandial serum triglyceride levels in mice by inhibiting lipase activity. Rhodionin also binds directly to SrtA to inhibit its transpeptidase activity, thereby reducing the fibrinogen adhesion and surface protein A levels of MRSA, effectively inhibiting biofilm formation and protecting against MRSA-induced cell damage. Rhodionin improves the survival rate of infected mice without affecting MRSA growth, and finds wide application in studies related to hyperlipidemia, exogenous obesity, and pneumonia induced by methicillin-resistant Staphylococcus aureus (MRSA).

Peonidin-3-O-galactoside chloride is an anthocyanin with antioxidant properties and blood-brain barrier permeability. Peonidin-3-O-galactoside chloride inhibits pancreatic lipase, with an IC₅₀ value of 23.2 μg/mL against porcine pancreatic lipase. Peonidin-3-O-galactoside chloride mediates neuroprotection, regulates glucose metabolism, protects cells from high glucose-induced damage, promotes glucose uptake and increases ATP production. Peonidin-3-O-galactoside (chloride) can be used in the research of obesity and neurodegenerative diseases.

(+)-Camphor-10-sulfonic acid ((+)-10-Camphorsulfonic acid) is an effective pancreatic lipase (PL) inhibitor. (+)-Camphor-10-sulfonic acid is promising for research of obesity.

HSL-IN-3 is a HSL inhibitor. HSL-IN-3 serves as an important intermediate for the synthesis of PARP-1 inhibitors. HSL-IN-3 can be used in studies related to lipid metabolism.

Cetilistat (ATL-962), an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC₅₀s of 54.8 nM, and 5.95 nM, respectively.

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.

HSL-IN-5 (Example 21) is a hormone sensitive lipase (HSL) inhibitor (IC₅₀: 0.25 μM). HSL-IN-5 can be used for diabetes research.

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC₅₀ values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y₁₄R (IC₅₀ = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.

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