| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Lysosomal acid lipase (LAL). It shows no significant activity against pancreatic lipase or lipoprotein lipase, indicating high specificity for its target.
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| ln Vitro |
Lalistat 2 inhibits purified human LAL with an IC50 of 152 nM. It does not significantly inhibit human pancreatic lipase or bovine milk lipoprotein lipase at concentrations up to 10 μM. At concentrations of 0.1-100 μM, it dose-dependently inhibits neutral lipid hydrolase activity in bone marrow-derived macrophages (BMDM). In HeLa cells preloaded with fatty acids, it blocks lipid clearance induced by autophagy enhancers.
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| ln Vivo |
Lalistat 2 has been used as a LAL inhibitor to study its effects on hypoxia-inducible factor (HIF) in mice. By inhibiting LAL, it alters lipid droplet morphology and localization in vivo, providing a model for studying the physiological consequences of LAL deficiency.
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| Enzyme Assay |
A typical in vitro enzyme assay uses purified human LAL and a fluorogenic substrate. The enzyme is incubated with varying concentrations of Lalistat 2, and the remaining activity is measured. The IC50 value is determined by plotting the percent inhibition against the log of inhibitor concentration. Pancreatic lipase and lipoprotein lipase are tested similarly to confirm the compound's specificity.
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| Cell Assay |
To study its cellular effects, cells such as BMDM or HeLa cells are cultured and treated with Lalistat 2 (e.g., 0.1-100 μM for 20 h). Lipid accumulation is assessed using techniques like Oil Red O staining or by measuring the levels of neutral lipids. Cell viability is also monitored to ensure the observed effects are not due to cytotoxicity.
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| Animal Protocol |
For in vivo studies, Lalistat 2 is typically administered to mice via intraperitoneal injection. The dosage and regimen vary depending on the experimental objective. For example, it can be used to study the effects of LAL inhibition on lipid metabolism and HIF pathways. Tissue samples are then collected for biochemical and histological analysis to evaluate lipid accumulation and other metabolic changes.
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| ADME/Pharmacokinetics |
Data on the pharmacokinetic properties of Lalistat 2 are limited as it is primarily a research tool. However, its solubility in DMSO (2 mg/mL) and its stability as a powder (store at 2-8°C) are documented. As a small molecule, its absorption, distribution, metabolism, and excretion (ADME) would be subject to standard metabolic pathways.
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| Toxicity/Toxicokinetics |
Based on available hazard classifications, Lalistat 2 is classified as Acute Tox. 4 Oral, indicating it may be harmful if swallowed. It requires standard laboratory safety precautions for handling. Specific toxicological data beyond this classification are not extensively detailed in general reference materials.
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| References |
[1]. Hamilton J, et al. A new method for the measurement of lysosomal acid lipase in dried blood spots using the inhibitor Lalistat 2. Clin Chim Acta. 2012;413(15-16):1207-1210.
[2]. Lukacs Z, et al. Best practice in the measurement and interpretation of lysosomal acid lipase in dried blood spots using the inhibitor Lalistat 2. Clin Chim Acta. 2017;471:201-205. |
| Additional Infomation |
Lalistat 2 is exclusively a research compound and is not approved for therapeutic use. Its primary application is as a chemical probe to investigate the role of LAL in various biological processes, including lipid metabolism, immune cell function, and lysosomal storage disorders. It is a valuable tool for studying the pathophysiology of diseases like Wolman disease and CESD.
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| Molecular Formula |
C13H20N4O2S
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|---|---|
| Molecular Weight |
296.39
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| Exact Mass |
296.13
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| CAS # |
1234569-09-5
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| PubChem CID |
46867138
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
438.5±45.0 °C at 760 mmHg
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| Flash Point |
219.0±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.586
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| LogP |
3.29
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
332
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(CC1)C2=NSN=C2OC(=O)N3CCCCC3
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| InChi Key |
PNYYVHOTXOEBEV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H20N4O2S/c18-13(17-9-5-2-6-10-17)19-12-11(14-20-15-12)16-7-3-1-4-8-16/h1-10H2
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| Chemical Name |
(4-piperidin-1-yl-1,2,5-thiadiazol-3-yl) piperidine-1-carboxylate
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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) |
DMSO: ≥ 100 mg/mL (337.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3739 mL | 16.8697 mL | 33.7393 mL | |
| 5 mM | 0.6748 mL | 3.3739 mL | 6.7479 mL | |
| 10 mM | 0.3374 mL | 1.6870 mL | 3.3739 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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