| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Lipoprotein lipase targets the core triglycerides of lipoproteins. Its physiological target is the ester bond in triglycerides. It requires the cofactor apolipoprotein C-II (ApoC-II) for full enzymatic activity. LPL is a key molecular target for drugs aimed at managing hypertriglyceridemia and reducing the risk of cardiovascular disease, particularly obesity and diabetes-related metabolic disorders.
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| ln Vitro |
In vitro, Lipoprotein lipase activity can be measured using artificial substrates like p-nitrophenyl butyrate. One unit of activity is defined as the amount of enzyme that releases 1.0 nmole of p-nitrophenol per minute at pH 7.2 and 37degC. It is also highly active against its natural substrates, chylomicrons and VLDL. The enzyme's activity is measured to assess its functional status or to screen for inhibitors.
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| ln Vivo |
In vivo, LPL is the rate-limiting enzyme for the clearance of triglyceride-rich lipoproteins from the bloodstream. It provides free fatty acids, which are a major energy source for the heart and skeletal muscle, and for storage in adipose tissue. Dysfunction of LPL leads to severe hypertriglyceridemia and an increased risk of pancreatitis and cardiovascular disease, making it a critical target for therapeutic intervention.
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| Enzyme Assay |
For in vitro (non-cellular) experiments, LPL activity is measured in a cell-free system. The enzyme is incubated with a substrate, such as a radiolabeled triolein emulsion or a chromogenic substrate like p-nitrophenyl butyrate, in a buffer containing albumin. The reaction is carried out at 37degC. The released free fatty acids are then extracted and quantified by liquid scintillation counting, or the release of p-nitrophenol is measured spectrophotometrically at 405 nm.
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| Cell Assay |
For in vitro cell-based experiments, cells that naturally express LPL, such as adipocytes or cardiomyocytes, are cultured in standard media. The cells are treated with compounds to either inhibit or stimulate LPL expression or activity. LPL activity can then be measured in the cell lysates or in the media after the cells are treated with heparin (which releases LPL from the cell surface), using the same in vitro enzymatic assays described above.
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| Animal Protocol |
For in vivo animal experiments, LPL function is often assessed in rodents. After an overnight fast, the animal can be injected intravenously with a fat emulsion (e.g., Intralipid). Blood samples are taken at various time points to measure plasma triglyceride clearance. The rate of clearance reflects the functional capacity of LPL. Additionally, tissues like muscle and adipose can be harvested post-mortem to measure LPL enzyme activity directly.
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| ADME/Pharmacokinetics |
As an endogenous enzyme, LPL has no pharmacokinetic (PK) profile as a drug. Its availability at the capillary endothelium is regulated by complex mechanisms including gene expression, protein synthesis, and translocation. The half-life of the active LPL protein at its site of action is relatively short, on the order of minutes to a few hours. It is degraded locally. Its activity is modulated by factors like insulin and nutritional status.
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| Toxicity/Toxicokinetics |
Lipoprotein lipase is an endogenous enzyme and is not inherently toxic. However, a deficiency in LPL activity leads to hypertriglyceridemia and can cause painful xerosis. Conversely, overwhelming the system with activators or inhibitors could lead to metabolic dysregulation. As a research reagent, it is generally considered non-hazardous, and standard laboratory precautions for handling biological proteins are sufficient.
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| References | |
| Additional Infomation |
hydrolytic enzyme that catalyzes the reaction of triglycerides with water to produce diglycerides and fatty acid anions. This enzyme hydrolyzes triglycerides in chylomicrons, very low-density lipoproteins, low-density lipoproteins, and diglycerides. It is present on the surface of capillary endothelium, especially in mammary glands, muscle, and adipose tissue. A genetic defect in this enzyme leads to familial hyperlipoproteinemia type I. (Dorland, 27th edition) EC 3.1.1.34.
Lipoprotein lipase is not a drug but a native, purified enzyme used extensively in research and in some diagnostic applications. It is used to measure triglyceride levels in clinical chemistry analyzers. It is also a major therapeutic target; drugs like fibrates that activate LPL are used to lower triglycerides. LPL is crucial for understanding the pathophysiology of obesity, dyslipidemia, and atherosclerosis, making it a key target for drug development. |
| Exact Mass |
2776.013
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|---|---|
| CAS # |
9004-02-8
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| PubChem CID |
167312575
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
27
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| Rotatable Bond Count |
70
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| Heavy Atom Count |
176
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| Complexity |
2530
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CC(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)F.CC(C)CC(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)F.CC(C)CC(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)Cl.CC(C)CC(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)Cl.CC(C)CC(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)Br.CC(C)C(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)C(C)(C)C.CC(C)C(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)F.CC(C)C(CCCCS(=O)(=O)O)C=CC1=CC=C(C=C1)Br
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| InChi Key |
JVCNNQAORSRACF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H32O3S.C17H25BrO3S.2C17H25ClO3S.2C17H25FO3S.C16H23BrO3S.C16H23FO3S/c1-16(2)18(8-6-7-15-24(21,22)23)12-9-17-10-13-19(14-11-17)20(3,4)5;5*1-14(2)13-16(5-3-4-12-22(19,20)21)7-6-15-8-10-17(18)11-9-15;2*1-13(2)15(5-3-4-12-21(18,19)20)9-6-14-7-10-16(17)11-8-14/h9-14,16,18H,6-8,15H2,1-5H3,(H,21,22,23);5*6-11,14,16H,3-5,12-13H2,1-2H3,(H,19,20,21);2*6-11,13,15H,3-5,12H2,1-2H3,(H,18,19,20)
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| Chemical Name |
5-[2-(4-bromophenyl)ethenyl]-7-methyloctane-1-sulfonic acid;7-(4-bromophenyl)-5-propan-2-ylhept-6-ene-1-sulfonic acid;7-(4-tert-butylphenyl)-5-propan-2-ylhept-6-ene-1-sulfonic acid;5-[2-(4-chlorophenyl)ethenyl]-7-methyloctane-1-sulfonic acid;5-[2-(4-fluorophenyl)ethenyl]-7-methyloctane-1-sulfonic acid;7-(4-fluorophenyl)-5-propan-2-ylhept-6-ene-1-sulfonic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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