| Size | Price | Stock | Qty |
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| Targets |
Lactupicrin targets multiple enzymes and pathways. It inhibits acetylcholinesterase (AChE), an enzyme that breaks down acetylcholine, with an IC₅₀ of 150.3 µM. It inhibits yeast alpha-glucosidase with an IC₅₀ of 14.71 µM. The compound inhibits NF-κB activation and LDLR1 generation, suggesting anti-inflammatory and atheroprotective mechanisms. Its targets include enzymes involved in neurotransmission, carbohydrate metabolism, and inflammatory signaling pathways.
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| ln Vitro |
In vitro, lactupicrin inhibits acetylcholinesterase (AChE) with an IC₅₀ of 150.3 µM and inhibits yeast alpha-glucosidase with an IC₅₀ of 14.71 µM. It inhibits NF-κB activation and LDLR1 generation, suggesting anti-inflammatory and atheroprotective activities. The compound exhibits analgesic and sedative activities, likely mediated through its effects on neurotransmitter systems and inflammatory pathways. Specific in vitro activities have been characterized in enzyme inhibition and cell-based assays.
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| ln Vivo |
In vivo, lactupicrin exhibits analgesic, sedative, antimalarial, and atheroprotective activities. It can relieve pain and has demonstrated protective effects against atherosclerosis. The compound's sedative effects suggest potential applications in anxiety and sleep disorders. Its antimalarial activity indicates potential for infectious disease research. Detailed in vivo efficacy data are limited in the available literature.
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| Enzyme Assay |
Non-cellular assays for lactupicrin would involve enzyme inhibition studies. Acetylcholinesterase inhibition can be assessed using the Ellman's assay, measuring the hydrolysis of acetylthiocholine. Alpha-glucosidase inhibition can be assessed using p-nitrophenyl-α-D-glucopyranoside as a substrate, measuring the release of p-nitrophenol. NF-κB inhibition can be studied using electrophoretic mobility shift assays (EMSA) or DNA binding assays in cell-free systems.
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| Cell Assay |
Cell-based assays for lactupicrin would involve evaluating its anti-inflammatory and analgesic activities. NF-κB activation can be assessed in immune cells using luciferase reporter assays or Western blot analysis of phosphorylated IκB. Anti-inflammatory activity can be evaluated by measuring cytokine production in LPS-stimulated macrophages. Analgesic activity could be studied in neuronal cell models. Specific protocols for these assays are not extensively documented in the available literature.
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| Animal Protocol |
In vivo animal studies for lactupicrin would typically involve pain models such as the hot plate test or formalin test to evaluate analgesic activity. Sedative effects could be assessed in open field or elevated plus maze tests. Antimalarial activity could be evaluated in Plasmodium-infected mouse models. Atheroprotective effects could be studied in ApoE-deficient mouse models of atherosclerosis. Specific protocols for these studies are not extensively documented in the search results.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for lactupicrin have not been reported in the available literature. As a sesquiterpene lactone with a molecular weight of 410.42 g/mol, its absorption, distribution, metabolism, and excretion would depend on its physicochemical properties. No specific pharmacokinetic parameters have been characterized for this compound.
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| Toxicity/Toxicokinetics |
No toxicity data have been reported for lactupicrin in the available literature. As a natural product found in chicory, it is generally considered to have a favorable safety profile, though systematic toxicological evaluation has not been performed. The compound is for research use only and is not for human therapeutic use. Standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
Lactucopicrin is an azurofuran compound belonging to the cyclic terpenoid ketones, enones, phenolic compounds, sesquiterpene lactones, and primary alcohols. It is a plant metabolite with sedative and antimalarial activities. Its function is related to 4-hydroxyphenylacetic acid and Lactucopicrin. Lactucopicrin has been reported in chicory (Cichorium spinosum), willowleaf lettuce (Lactuca saligna), and other organisms with relevant data.
Lactupicrin is a research compound and natural product, not an approved pharmaceutical drug. It is a characteristic bitter sesquiterpene lactone found in chicory and other plants. The compound exhibits analgesic, sedative, antimalarial, and atheroprotective activities. It inhibits AChE (IC₅₀ = 150.3 µM), alpha-glucosidase (IC₅₀ = 14.71 µM), and NF-κB activation. It is used as an analytical standard and in natural product research. Lactupicrin is for research use only. |
| Molecular Formula |
C23H22O7
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|---|---|
| Molecular Weight |
410.42
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| Exact Mass |
410.137
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| CAS # |
65725-11-3
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| PubChem CID |
174880
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| Appearance |
White to off-white solid
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| LogP |
1.782
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
844
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=C2C(C3C(C(C1)OC(=O)CC4=CC=C(C=C4)O)C(=C)C(=O)O3)C(=CC2=O)CO
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| InChi Key |
UMVSOHBRAQTGQI-XGARDCMYSA-N
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| InChi Code |
InChI=1S/C23H22O7/c1-11-7-17(29-18(27)8-13-3-5-15(25)6-4-13)20-12(2)23(28)30-22(20)21-14(10-24)9-16(26)19(11)21/h3-6,9,17,20-22,24-25H,2,7-8,10H2,1H3/t17-,20+,21-,22-/m0/s1
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| Chemical Name |
[(3aR,4S,9aS,9bR)-9-(hydroxymethyl)-6-methyl-3-methylidene-2,7-dioxo-4,5,9a,9b-tetrahydro-3aH-azuleno[4,5-b]furan-4-yl] 2-(4-hydroxyphenyl)acetate
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| Synonyms |
Lactupicrin; Lactucopicrin
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 250 mg/mL (609.13 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 | 2.4365 mL | 12.1826 mL | 24.3653 mL | |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4365 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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