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Pancreatic lipase/Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A) with IC50 values of 2.13 µM and 0.055 µM against PL and hCES1A .
Triacylglycerol lipase is an enzyme that preferentially hydrolyzes the outer links of triacylglycerols and acts only on the water-lipid interface. Pancreatic triacylglycerol lipase is the single most important determinant of lipid absorption .
Lipoprotein lipase, Pseudomonas sp (LPL) is a multifunctional enzyme from adipose tissue, heart and skeletal muscle, islets and macrophages. Lipoprotein lipase promotes normal lipoprotein metabolism, delivery and utilization of tissue-specific substrates. Lipoprotein lipase catalyzes the rate-limiting step of lipids in blood circulation .
4-Methylumbelliferyl oleate is a fluorogenic substrate for acid and alkaline lipases. 4-Methylumbelliferyl oleate is cleaved by lipases, liberating 4-Methylumbelliferyl (Ex/Em=320/450 nm) .
Ciwujianoside C2 is a saponin, that can be isolated from the leaves of Acanthopanax senticosus. Ciwujianoside C2 enhances pancreatic lipase activity in vitro .
1-Isomangostin is an inhibitor of pancreatic lipase. 1-Isomangostin inhibits porcine pancreatic lipase with an IC50 of 34.5 μM. 1-Isomangostin has anti-obesity activity .
Ciwujianoside C1 is a saponin, that can be isolated from the leaves of Acanthopanax senticosus. Ciwujianoside C1 inhibits pancreatic lipase activity in vitro .
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 .
Cetilistat impurity 1 is an impurity of Cetilistat. Cetilistat, 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 .
Lubabegron (LY-488756) fumarate is an antagonist of the adrenergic receptor (β-AR). Lubabegron fumarate can antagonize the stimulatory effects of β1-AR and β2-AR agonists on lipase respectively .
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 .
Uvagrandol potently inhibits α-glucosidase and porcine lipase (IC50: 15.2 μM, 11.2 μM respectively). Uvagrandol can be used in the research of Type 2 diabetes and obesity .
Mono-and diglycerides is formed by triglycerides being broken down by pancreatic lipase in the gastrointestinal lumen. Mono-and diglycerides is a food additive used as a nonionic emulsifier and mainly present in food fats .
5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) can be isolated from Dendrobium infundibulum (D. infundibulum). 5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl has no inhibitory activity against α-glucosidase and pancreatic lipase .
Echitamine (Ditaine) chloride is the major monoterpene indole alkaloid present in Alstonia scholaris with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 μM .
(1,5E,11E)-Tridecatriene-7,9-diyne-3,4-diacetate, isolated from the ethanol extract of Atractylodes lancea rhizome, displays significant lipase inhibition with an IC50 value of 23.9 µg/mL. Antiobesity Effect .
H-Pro-Glu-OH is a protein secreted by pathogenic mycobacteria through the Type VII secretion system. H-Pro-Glu-OH targets LipY lipases to the cell Surface via the ESX-5 Pathway .
4-Methylumbelliferyl palmitate is an excellent fluorophore for measuring acid lipase in human leukocytes. Acidity and solvent have important influence on its fluorescence. 4-Methylumbelliferyl palmitate exists mainly as neutral molecular form which can be produced strong fluorescence at 445 nm in near neutral aqueous solutions, and exist mainly as anion form which can be produced stronger fluorescence at 445 nm in weak alkaline solutions .
MAGL-IN-10 is areversible monoacylglycerol lipase (MAGL) inhibitor with very good ADME properties and low in vivo toxicity.MAGL-IN-10 can be used for the research ofcancer, neurological disorders and inflammatory pathologies .
Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity . Anti-atherosclerotic effect .
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC) .
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
MAGL-IN-5 (CAY10499) is a non-selective lipase inhibitor with IC50 values of 144, 90, and 14 nM for human recombinant monoacylglycerol lipase(MAGL),hormone sensitive lipase(HSL), and fatty acid amide hydrolase(FAAH) respectively .
LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [ 14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM .
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
Lalistat 2 is an inhibitor of many lipases especially Lysosomal acid lipase (LAL, IC50 = 152 nM), which is a key enzyme that degrades neutral lipids at an acidic pH in lysosomes. Lalistat 2 is commonly used to investigate the cell-specific functions of LAL and LAL deficiency in vitro, as well as specifically measure LAL activity in human blood samples or cells .
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
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 .
JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively .
MAGL-IN-13 (compound (3R, 4S) - 5v) is a selective, irreversible inhibitor for MAGL,with IC50 values of 0.026, 0.021 and 0.24 nM for mMAGL, hMAGL and rMAGL, respectively. MAGL-IN-13 can penetrant blood brain barrier. .
DAGLβ-IN-1 is an inhibitor of diacylglycerol lipase-β (DAGLβ), serves as a versatile intermediate for the design of DAGL-tailored activity-based probes .
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 .
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
hPL-IN-2 (compound 2u) is a potent, reversible, and non-competitive inhibitor of pancreatic lipase (IC50: 1.63 μM) and can be used in anti-obesity research .
4-Nitrophenyl stearate, which is an ester formed by the condensation of stearic acid and 4-nitrophenol, is commonly used as a substrate for enzymatic assays, where the hydrolysis of ester bonds by esterase and lipase can be measured by absorbance or ratio In addition, 4-Nitrophenyl stearate has been used as a model compound to study the enzymatic activity and selectivity of lipases and esterases from various sources. The long hydrophobic tail of the molecule makes it suitable for use in lipophilic Good solubility in the environment makes it a useful probe for studying lipid metabolism.
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 .
Oleoyl coenzyme A triammonium is the salt form of Oleoyl coenzyme A, which exhibits an inhibitory effects for neutral lipase. Oleoyl coenzyme A triammonium mediates ATP-dependent signal transduction pathway in plants .
3-O-Methylgalangin (Galangin 3-methyl ether) is a natural flavonoid compound from the rhizome of Alpinia officinarum (AO) with antibacterial activities, which also inhibits pancreatic lipase .
Undecanoic acid-d21 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Undecanoic acid-d3 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Undecanoic acid-d2 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Sanggenon D is a Diels-Alder-type adduct from Chinese crude agent root bark of mulberry ( Morus alba L.). Sanggenon D possesses antioxidant and inhibits Pancreatic lipase (PL) with the an IC50 of 0.77 μM.
NG-497 is a selective human adipose triglyceride lipase (ATGL) inhibitor that targets the enzymatically active patatin-like domain of human ATGL. NG-497 has potential value for tumor research .
Undecanoic acid (Standard) is the analytical standard of Undecanoic acid. This product is intended for research and analytical applications. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
DDAO is a promising near-infrared (NIR) red fluorescent probewith tunable excitation wavelength (600-650nm) and longemission wavelength(λem=656nm). DDAO can de desiged for detection of the activities of different enzymes such asβ-galactosidase,sulfatase, proteinphosphatase2A,carboxylesterase 2, humanalbumin andesterases .
UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase .
JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL) .
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed proagent of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects .
FAAH/MAGL-IN-4 (Compound 13) is a potent fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) inhibitor with IC50s of 9.1 nM and 7.9 μM, respectively. FAAH/MAGL-IN-4 can be used for the research of pain and CNS disorders .
Cholesterol esterase, Pseudomonas is an enzyme that hydrolyzes cholesterol ester to cholesterol and free fatty acid in the intestinal lumen. Cholesterol synthesized in the acinar cells and is stored in zymogen granules. Cholesterol esterase is also known as bile salt-stimulated lipase and carboxy ester lipasea, acts function for acceleration of cholesterol absorption .
MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively . MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity .
Orlistat (Standard) is the analytical standard of Orlistat. This product is intended for research and analytical applications. Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity .?Anti-atherosclerotic?effect .
5-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes .
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits cutinase, exhibits plants protective potency against Erysiphe graminis .
6-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes .
5(6)-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes .
FP-biotin is a potent organophosphorus toxicant, well-suited for searching for new biomarkers of organophosphorus toxicants exposure. FP-Biotin quantifies FAAH, ABHD6, and MAG-lipase activity. FP-biotin is used for studies with plasma because biotinylated peptides are readily purified by binding to immobilized avidin beads .
DDAO-C6 is a cridone ester derivative, highly specific fluorescence for detecting human serum albumin (HSA). DDAO-C6 acts as an enzymatic activatable near-infrared fluorescent probe in visually sensing endogenous lipase from gut microbes (Ex/Em=600/658 nm) .
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .
MGL-IN-1 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. MGL-IN-1 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. MGL-IN-1 displays high membrane permeability and brain penetrant .
ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors .
Lipstatin is a pancreatic lipase inhibitor (IC50=0.14 μM), whose structure is closely related to the known inhibitor, Esterastin. Lipstatin inhibits the absorption of triglycerides without affecting the absorption of oleic acid. Lipstatin has no inhibitory effects on other pancreatic enzymes, such as phospholipase A2 and trypsin (<200 μM) .
Epitheaflagallin 3-O-gallate is a minor polyphenol in black tea. Epitheaflagallin 3-O-gallate exhibits versatile physiological functions in vivo and in vitro, including antioxidative activity, pancreatic lipase inhibition, Streptococcus sorbinusglycosyltransferase inhibition, and an inhibiting effect on the activity of matrix metalloprotease-1 and -3 and their synthesis by human gingival fibroblasts .
O-7460 is a potent and selective DAGLα inhibitor, with an IC50 of 0.69 μM. O-7460 shows selectivity over onoacylglycerol lipase (MAGL), human CB1 and CB2 cannabinoid receptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels .
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice . DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
Poloxamer 407 (F127) is a nonionic surfactant that is 100% active and relatively non-toxic to cells at low concentrations, and frequently used with dye AM esters such as Indo-1 AM, Fura-2 AM, Calcein AM, Fluo-3 AM, Fluo-4 AM, Quest Fluo-8™ AM and Quest Rhod-4™ AM, etc. to improve their water solubility. Poloxamer 407 is also a lipoprotein lipase inhibitor .
4-Nitrophenyl butyrate consists of butyric acid chains esterified with 4-nitrophenol groups, thus giving it a yellow color. This compound is commonly used as a substrate in enzyme assays to measure esterase and lipase activity. When these enzymes cleave the ester bond, the nitrophenol group is released and the color changes from yellow to orange. Thus, the rate of color change can be used to determine enzyme activity. In addition, 4-Nitrophenyl butyrate can also be used as organic synthesis reagent and dye intermediate.
7-Hydroxycoumarinyl arachidonate (7-HCA) is a fluorogenic substrate of cytosolic phospholipase A2 (PLA2). 7-Hydroxycoumarinyl arachidonate is also a fluorogenic substrate for monoacylglycerol lipase (MAGL). MAGL protein catalyzes the hydrolysis of 7-Hydroxycoumarinyl arachidonat to generate Arachidonic acid (AA) and the highly fluorescent 7-hydroxyl coumarin (7-HC; HY-N0573). Release of 7-HC can be measured using a fluorometer .
(Z)-KC02 is an inhibitor of ABHD16A, the phosphatidylserine (PS) lipase that produces lyso-PS. Lysophosphatidylserine (lyso-PS) is a signaling lipid that regulates immune and neurological processes. It is associated with several neurological disorders such as retinitis pigmentosa and cataracts (PHARC). (Z)-KC02 depletes lyso-PS in lymphoblasts from PHARC subjects. (Z)-KC02 also reduces lyso-PS and lipopolysaccharide-induced cytokine production in macrophages and modulates lyso-PS metabolism in vivo .
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats .
LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research .
KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages .
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
4-Methylumbelliferyl palmitate is an excellent fluorophore for measuring acid lipase in human leukocytes. Acidity and solvent have important influence on its fluorescence. 4-Methylumbelliferyl palmitate exists mainly as neutral molecular form which can be produced strong fluorescence at 445 nm in near neutral aqueous solutions, and exist mainly as anion form which can be produced stronger fluorescence at 445 nm in weak alkaline solutions .
DDAO is a promising near-infrared (NIR) red fluorescent probewith tunable excitation wavelength (600-650nm) and longemission wavelength(λem=656nm). DDAO can de desiged for detection of the activities of different enzymes such asβ-galactosidase,sulfatase, proteinphosphatase2A,carboxylesterase 2, humanalbumin andesterases .
5-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes .
6-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes .
5(6)-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes .
DDAO-C6 is a cridone ester derivative, highly specific fluorescence for detecting human serum albumin (HSA). DDAO-C6 acts as an enzymatic activatable near-infrared fluorescent probe in visually sensing endogenous lipase from gut microbes (Ex/Em=600/658 nm) .
4-Nitrophenyl stearate, which is an ester formed by the condensation of stearic acid and 4-nitrophenol, is commonly used as a substrate for enzymatic assays, where the hydrolysis of ester bonds by esterase and lipase can be measured by absorbance or ratio In addition, 4-Nitrophenyl stearate has been used as a model compound to study the enzymatic activity and selectivity of lipases and esterases from various sources. The long hydrophobic tail of the molecule makes it suitable for use in lipophilic Good solubility in the environment makes it a useful probe for studying lipid metabolism.
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
Poloxamer 407 (F127) is a nonionic surfactant that is 100% active and relatively non-toxic to cells at low concentrations, and frequently used with dye AM esters such as Indo-1 AM, Fura-2 AM, Calcein AM, Fluo-3 AM, Fluo-4 AM, Quest Fluo-8™ AM and Quest Rhod-4™ AM, etc. to improve their water solubility. Poloxamer 407 is also a lipoprotein lipase inhibitor .
4-Nitrophenyl butyrate consists of butyric acid chains esterified with 4-nitrophenol groups, thus giving it a yellow color. This compound is commonly used as a substrate in enzyme assays to measure esterase and lipase activity. When these enzymes cleave the ester bond, the nitrophenol group is released and the color changes from yellow to orange. Thus, the rate of color change can be used to determine enzyme activity. In addition, 4-Nitrophenyl butyrate can also be used as organic synthesis reagent and dye intermediate.
(Z)-KC02 is an inhibitor of ABHD16A, the phosphatidylserine (PS) lipase that produces lyso-PS. Lysophosphatidylserine (lyso-PS) is a signaling lipid that regulates immune and neurological processes. It is associated with several neurological disorders such as retinitis pigmentosa and cataracts (PHARC). (Z)-KC02 depletes lyso-PS in lymphoblasts from PHARC subjects. (Z)-KC02 also reduces lyso-PS and lipopolysaccharide-induced cytokine production in macrophages and modulates lyso-PS metabolism in vivo .
Rimtoregtide is a polypeptide compound which significantly reduces the increase in the levels of amylase and lipase in the blood caused by acute pancreatitis. Rimtoregtide has the potential for the research of pancreatitis and acute pancreatitis (extracted from patent WO2018205233A1).
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
Ciwujianoside C2 is a saponin, that can be isolated from the leaves of Acanthopanax senticosus. Ciwujianoside C2 enhances pancreatic lipase activity in vitro .
1-Isomangostin is an inhibitor of pancreatic lipase. 1-Isomangostin inhibits porcine pancreatic lipase with an IC50 of 34.5 μM. 1-Isomangostin has anti-obesity activity .
Ciwujianoside C1 is a saponin, that can be isolated from the leaves of Acanthopanax senticosus. Ciwujianoside C1 inhibits pancreatic lipase activity in vitro .
Uvagrandol potently inhibits α-glucosidase and porcine lipase (IC50: 15.2 μM, 11.2 μM respectively). Uvagrandol can be used in the research of Type 2 diabetes and obesity .
5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) can be isolated from Dendrobium infundibulum (D. infundibulum). 5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl has no inhibitory activity against α-glucosidase and pancreatic lipase .
Echitamine (Ditaine) chloride is the major monoterpene indole alkaloid present in Alstonia scholaris with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 μM .
(1,5E,11E)-Tridecatriene-7,9-diyne-3,4-diacetate, isolated from the ethanol extract of Atractylodes lancea rhizome, displays significant lipase inhibition with an IC50 value of 23.9 µg/mL. Antiobesity Effect .
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
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 .
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 .
3-O-Methylgalangin (Galangin 3-methyl ether) is a natural flavonoid compound from the rhizome of Alpinia officinarum (AO) with antibacterial activities, which also inhibits pancreatic lipase .
Sanggenon D is a Diels-Alder-type adduct from Chinese crude agent root bark of mulberry ( Morus alba L.). Sanggenon D possesses antioxidant and inhibits Pancreatic lipase (PL) with the an IC50 of 0.77 μM.
Undecanoic acid (Standard) is the analytical standard of Undecanoic acid. This product is intended for research and analytical applications. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits cutinase, exhibits plants protective potency against Erysiphe graminis .
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .
Epitheaflagallin 3-O-gallate is a minor polyphenol in black tea. Epitheaflagallin 3-O-gallate exhibits versatile physiological functions in vivo and in vitro, including antioxidative activity, pancreatic lipase inhibition, Streptococcus sorbinusglycosyltransferase inhibition, and an inhibiting effect on the activity of matrix metalloprotease-1 and -3 and their synthesis by human gingival fibroblasts .
Gastric lipase is a key enzyme in the digestive process and plays a key role in the hydrolysis of triacylglycerols into free fatty acids, diacylglycerols, monoacylglycerols, and glycerol. This enzyme activity contributes significantly to the breakdown of dietary fat in the gastric environment. Gastric lipase Protein, Human (HEK293, His) is the recombinant human-derived Gastric lipase protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Gastric lipase Protein, Human (HEK293, His) is 379 a.a., with molecular weight of ~53.85 kDa.
Gastric lipase is a key enzyme in the digestive process and plays a key role in the hydrolysis of triacylglycerols into free fatty acids, diacylglycerols, monoacylglycerols, and glycerol. This enzyme activity contributes significantly to the breakdown of dietary fat in the gastric environment. Gastric lipase Protein, Human (HEK293, C-His) is the recombinant human-derived Gastric lipase protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Gastric lipase Protein, Human (HEK293, C-His) is 379 a.a., with molecular weight of ~48.09 kDa.
PNLIP/Pancreatic lipase Protein is pivotal in fat metabolism, preferentially cleaving esters of long-chain fatty acids at positions 1 and 3, yielding 2-monoacylglycerol and free fatty acids. It displays increased activity with insoluble emulsified substrates over soluble ones. PNLIP/Pancreatic lipase Protein, Human (HEK293, His) is the recombinant human-derived PNLIP/Pancreatic lipase protein, expressed by HEK293 , with C-His, C-8*His labeled tag. The total length of PNLIP/Pancreatic lipase Protein, Human (HEK293, His) is 449 a.a., with molecular weight of ~51 kDa.
Monoglyceride lipase is a key enzyme in lipid metabolism and plays a key role in converting monoacylglycerols into free fatty acids and glycerol, contributing to important cellular processes. In addition to being involved in lipid metabolism, this enzyme also hydrolyzes the endocannabinoid 2-arachidonoylglycerol, thereby affecting the complex regulation of endocannabinoid signaling, nociception, and pain perception. Monoglyceride lipase Protein, Rat (P.pastoris, His) is the recombinant rat-derived Monoglyceride lipase protein, expressed by P. pastoris , with N-His labeled tag. The total length of Monoglyceride lipase Protein, Rat (P.pastoris, His) is 303 a.a., with molecular weight of ~35.5 kDa.
Pancreatic lipase (PNLIP) plays a crucial role in fat metabolism by enzymatically breaking down dietary lipids and preferentially selecting long-chain fatty acid esters at positions 1 and 3. This results in the production of mainly 2-monoacylglycerol and free fatty acids. PNLIP/Pancreatic lipase Protein, Mouse (His-SUMO) is the recombinant mouse-derived PNLIP/Pancreatic lipase protein, expressed by E. coli , with N-His, N-SUMO labeled tag. The total length of PNLIP/Pancreatic lipase Protein, Mouse (His-SUMO) is 449 a.a., with molecular weight of ~65.8 kDa.
Carboxyester lipase/CEL protein plays a crucial role in cellular processes as it catalyzes the hydrolysis of a variety of substrates, including cholesterol esters, phospholipids, lysophospholipids, diacylglycerols and triacylglycerols, and lipids of hydroxy fatty acids acid ester. FAHF). Carboxyl Ester Lipase/CEL Protein, Mouse (sf9, His) is the recombinant mouse-derived Carboxyl Ester Lipase/CEL protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of Carboxyl Ester Lipase/CEL Protein, Mouse (sf9, His) is 534 a.a., with molecular weight of ~133.9 & 59.1 kDa, respectively.
MGLL proteins convert monoacylglycerides into free fatty acids and glycerol. MGLL Protein, Human is the recombinant human-derived MGLL protein, expressed by E. coli , with tag free. The total length of MGLL Protein, Human is 302 a.a., .
MGLL proteins convert monoacylglycerides into free fatty acids and glycerol. MGLL Protein, Human (His) is the recombinant human-derived MGLL protein, expressed by E. coli , with N-6*His labeled tag. The total length of MGLL Protein, Human (His) is 302 a.a., .
The PLRP2 protein is a multifunctional lipase that hydrolyzes triglycerides and galactosylglycerides with broad substrate specificity. It is essential for newborns and plays an important role in the pancreas' digestion of dietary fats, especially milk fat globules, which are rich in long-chain triglycerides. PLRP2 Protein, Human (sf9, His) is the recombinant human-derived PLRP2 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of PLRP2 Protein, Human (sf9, His) is 469 a.a., with molecular weight of ~57 kDa.
PLRP1 Protein is a protein that encoded by PNLIPRP1 genne. PLRP1 is produced by pancreatic acinar cells and expressed in the pancreas. PLRP1 is involved in lipid catabolic process, acting as a negative regulator of pancreatic lipase activity by competing with pancreatic lipase for colipase occupancy. And it may function as inhibitor of dietary triglyceride digestion. PLRP1 Protein, Human (HEK293, His) is the recombinant human-derived PLRP1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PLRP1 Protein, Human (HEK293, His) is 450 a.a., with molecular weight of 44-50 kDa.
The PNLIPRP1 protein acts as an inhibitor of dietary triglyceride digestion and lacks lipase activity on various substrates. This regulatory effect suggests an effect on the breakdown of dietary triglycerides. PNLIPRP1 Protein, Dog (P.pastoris, His) is the recombinant dog-derived PNLIPRP1 protein, expressed by P. pastoris , with N-His labeled tag. The total length of PNLIPRP1 Protein, Dog (P.pastoris, His) is 450 a.a., with molecular weight of ~51.7 kDa.
PNLIPRP1 Protein, a potential inhibitor of dietary triglyceride digestion, likely modulates lipid metabolism. In vitro analyses reveal its lack of detectable lipase activity, suggesting a unique role as an enzyme inhibitor rather than an active participant in triglyceride hydrolysis. This characteristic underscores PNLIPRP1's potential regulatory impact on lipid digestion processes. PNLIPRP1 Protein, Rat (HEK293, His) is the recombinant rat-derived PNLIPRP1 protein, expressed by HEK293 , with C-His labeled tag. The total length of PNLIPRP1 Protein, Rat (HEK293, His) is 456 a.a., with molecular weight of ~52 KDa.
ABHD4 is a lysophospholipase that acts selectively on N-acylphosphatidylethanolamines (NAPE), which is essential for the biosynthesis of N-acylphosphatidylethanolamines such as anandamide. It hydrolyzes the sn-1 and sn-2 acyl chains in NAPE to generate glycerophosphate-N-acylethanolamine (GP-NAE), which is an important intermediate in the production of N-acylethanolamine. ABHD4 Protein, Human (sf9, His) is the recombinant human-derived ABHD4 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of ABHD4 Protein, Human (sf9, His) is 342 a.a., with molecular weight of ~40 KDa.
The PNPLA2 protein catalyzes the hydrolysis of triglycerides, preferably long-chain fatty acid esters, in lipid droplets. PNPLA2 Protein, Human (His-SUMO) is the recombinant human-derived PNPLA2 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of PNPLA2 Protein, Human (His-SUMO) is 504 a.a., with molecular weight of ~71.3 kDa.
Undecanoic acid-d21 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Undecanoic acid-d3 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Undecanoic acid-d2 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Phospho-Hormone sensitive lipase (Ser853) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 117 kDa, targeting to Phospho-Hormone sensitive lipase (S853). It can be used for WB,IHC-P assays with tag free, in the background of Human, Mouse, Rat.
Adipose Triglyceride Lipase Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 55 kDa, targeting to Adipose Triglyceride Lipase. It can be used for WB assays with tag free, in the background of Human, Mouse, Rat.
DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice . DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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