| Size | Price | Stock | Qty |
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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 |
IC50: 68 nM ( human LAL)[1]
Lalistat 1 targets lysosomal acid lipase (LAL), an enzyme that hydrolyzes cholesteryl esters and triglycerides in lysosomes. By inhibiting LAL with an IC50 of 68 nM, Lalistat 1 blocks LAL-mediated lipid hydrolysis of acetylated LDL and reduces efflux of cholesterol from lipid-loaded cells. This makes it a valuable tool for studying lipid metabolism, cholesterol homeostasis, and lysosomal storage disorders such as Niemann-Pick type C disease. |
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| ln Vitro |
In Elisa assays, Lalistat 1 (0-100 μM) shown efficacy against several non-typeable H. IgAP variations from clinical isolates of H. influenzae (NTHi). IgA1P B1 and B2 were shown to be inhibited in a dose-dependent manner, although at greater inhibitor concentrations, which is in line with these variants' higher expression levels. IgA1P B1 and B2 were shown to be almost completely inhibited at 50 μM and completely inhibited at 100 μM [1].
In vitro, Lalistat 1 inhibits lysosomal acid lipase (LAL) with an IC50 of 68 nM using purified human LAL. It is selective for LAL over human pancreatic and bovine milk lipoprotein lipases up to 10 µM. Lalistat 1 (0.01-10 µM) reduces cholesterol accumulation in lysosome-like storage organelles in GM03123 human fibroblast cells deficient in NPC1. It has little effect on cholesterol accumulation in NPC1-deficient CHO cells. |
| ln Vivo |
In vivo data for Lalistat 1 is limited in publicly available sources. As a potent and selective LAL inhibitor, the compound has potential applications in animal models of Niemann-Pick type C disease and other lysosomal storage disorders. By modulating lipid metabolism and cholesterol homeostasis, Lalistat 1 could provide insights into the pathophysiology of these diseases. However, specific published in vivo efficacy studies are not detailed in the current literature. Lalistat 1 is primarily used as a research tool.
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| Enzyme Assay |
The in vitro LAL inhibition assay for Lalistat 1 uses purified human lysosomal acid lipase and a fluorogenic substrate. Enzyme activity is measured fluorometrically, and IC50 values are calculated from dose-response curves. Selectivity profiling against human pancreatic and bovine milk lipoprotein lipases is performed using similar assay formats. Cholesterol accumulation assays are performed in NPC1-deficient human fibroblasts treated with Lalistat 1 (0.01-10 µM).
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| Cell Assay |
Cellular assays for Lalistat 1 are conducted in NPC1-deficient human fibroblasts (GM03123) and CHO cells. Cells are treated with varying concentrations of Lalistat 1 (0.01-10 µM). Cholesterol accumulation in lysosome-like storage organelles is measured using filipin staining or biochemical assays. LAL activity is measured in cell lysates using fluorogenic substrates. Cell viability is assessed using standard assays. The compound's effects on lipid metabolism are evaluated by measuring lipid levels.
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| Animal Protocol |
In vivo studies for Lalistat 1 would typically involve mouse models of Niemann-Pick type C disease. The compound would be administered via intraperitoneal or oral routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring cholesterol accumulation in tissues, neurological function, and survival. However, specific published in vivo protocols for Lalistat 1 are not available in the current literature. The compound is currently used as a research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Lalistat 1 is not extensively reported in publicly available sources. The compound has a molecular weight of 298.36 g/mol and a molecular formula of C12H18N4O3S. It has a CAS number of 501104-16-1. It is soluble in DMF and DMSO at 20 mg/mL. Storage: -20°C. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for Lalistat 1 is limited in publicly available sources. As with all research compounds, Lalistat 1 is intended for research use only and not for human or veterinary use. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. The compound's mechanism of inhibiting lipid metabolism suggests potential effects on lipid homeostasis that would need to be evaluated.
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| References | |
| Additional Infomation |
Lalistat 1 (CAS 501104-16-1) is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) with an IC50 of 68 nM. It is selective for LAL over lipoprotein lipases up to 10 µM. Lalistat 1 reduces cholesterol accumulation in NPC1-deficient fibroblasts and is used in Niemann-Pick type C disease research. It has a molecular formula of C12H18N4O3S and a molecular weight of 298.36 g/mol.
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| Molecular Formula |
C12H18N4O3S
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|---|---|
| Molecular Weight |
298.361320972443
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| Exact Mass |
298.109
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| CAS # |
501104-16-1
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| PubChem CID |
651937
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| Appearance |
White to off-white solid powder
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
335
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C(OC2C(N3CCCCC3)=NSN=2)=O)CCOCC1
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| InChi Key |
XAWUWPUYJUOUOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H18N4O3S/c17-12(16-6-8-18-9-7-16)19-11-10(13-20-14-11)15-4-2-1-3-5-15/h1-9H2
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| Chemical Name |
(4-piperidin-1-yl-1,2,5-thiadiazol-3-yl) morpholine-4-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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : 20 mg/mL (67.03 mM )
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3517 mL | 16.7583 mL | 33.5166 mL | |
| 5 mM | 0.6703 mL | 3.3517 mL | 6.7033 mL | |
| 10 mM | 0.3352 mL | 1.6758 mL | 3.3517 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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