ラクチュコピクリン
Based on 1 Customer Validation
Lactupicrin (Lactucopicrin) exhibits analgesic, sedative, antimalarial activities and atheroprotective effect. Lactupicrin inhibits acetylcholinesterase (AChE) with an IC50 of 150.3 μM. Lactupicrin is an orally active characteristic bitter sesquiterpene lactone.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.62%
- CAS 番号: 65725-11-3
- 分子式: C23H22O7
- 分子量:410.42
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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生物活性
Lactupicrin (0.25-1 μM, 24 h) attenuates cholesterol influx into low-grade inflammatory macrophages by targeting LOX-1[2].
Lactupicrin (0.625-40 μM, 24 h) reduces NF-κB activities in inflammated macrophages[3].
Lactupicrin (40 μM, 24 h) inhibits p65 nuclear translocation by downregulation of cytoplasmic dynein-mediated transport of p65 in inflammated macrophages[3].
Lactupicrin (50 μg/L, 48 h) completely prevents parasite growth[4].
Lactupicrin (10-1000 μM, 45 min) exhibits AChE inhibition dose-dependently [4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:low-grade inflammatory macrophages
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:24 h
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Result:Did not form foam cell and cholesterol influx knocked down with LOX-1 and inhibited foam cell formation in cells knocked down with either SR-A or CD36.
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Cell Line:Bone marrow-derived macrophages (BMDMs).
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Concentration:10, 20, 40 μM
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Incubation Time:24 h
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Result:Significantly reduced nuclear p65 content at 20 and 40 μM.
Inhibited the interaction of cytoplasmic dynein with p65 at 40 μM.
Did not affect the expression of dynein at 10, 20, 40 μM.
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Cell Line:Bone marrow-derived macrophages (BMDMs) cells.
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Concentration:10, 20, 40 μM
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Incubation Time:24 h
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Result:Significantly reduced mRNA and protein levels of IL-1β, IL-6, and TNF-α, downstreams of NF-κB at 20 and 40 μM.
Did not affect the mRNA and protein expression of importin-α5 at 10-40 μM.
Did not affect the expression of dynein.
Lactupicrin (1.2-120 mg/kg, p.o., daily, 12 weeks) limits macrophage foam cell formation through a reduction of LOX-1 in lipid rafts, contributing to its atheroprotective effect in ApoE-/- mice[2].
Lactupicrin (1.2-120 mg/kg, p.o., daily, 12 weeks) inhibits early atherosclerosis formation in ApoE-/-mice[3].
Lactupicrin (1.2-120 mg/kg, p.o., daily, 12 weeks) reduces ApoE-/-mice serum levels of IL-1β and TNF-α but not IL-6 dose-dependently[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Albino Swiss mice, weighing 24-28 g[1].
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Dosage:15, 30 mg/kg
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Administration:i.p.
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Result:Prolonged the latency towards a noxious stimulus by 142 %.
Showed significant antinociceptive activities.
Decreased the spontaneous locomotor activity at a dose of 30 mg/kg (but not 15 mg/kg).
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Animal Model:ApoE-/- mice (C57BL/6), 8 weeks old, male, were fed with a high-fat diet (21% milk fat, 0.15% cholesterol)[2].
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Dosage:1.2, 12, 120 mg/kg
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Administration:p.o., daily, 12 weeks
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Result:Reduced the percentage of F4/80 (a marker to identify macrophage) positive derived foam cells within plaques at the aortic sinus dose-dependently.
Reduced the mRNA levels of Lox1 and F4/80 in aortic arches dose-dependently.
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Animal Model:Male ApoE-/- mice (C57BL/6), 6-8 weeks old, were fed a high fat diet (21% milk fat, 0.15% cholesterol)[3].
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Dosage:12, 120 mg/kg
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Administration:p.o., daily, 12 weeks
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Result:Reduced the atherosclerotic plaque area at the sites of both aortic sinus and thoracic and abdominal aortas.
Reduced the percentage of CD68 and F4/80 (two widely used markers to identify macrophages) positive cells within plaques at the aortic sinus.
化学情報
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CAS 番号 65725-11-3
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性状 Solid
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分子量 410.42
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分子式 C23H22O7
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Color White to off-white
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SMILES
OCC([C@](C1=C2C)([H])[C@](OC3=O)([H])[C@@](C3=C)([H])[C@H](C2)OC(CC(C=C4)=CC=C4O)=O)=CC1=O
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別名
Lactupicrin; Lactucopicrin
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 250 mg/mL (609.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wesołowska A, et, al. Analgesic and sedative activities of lactucin and some lactucin-like guaianolides in mice. J Ethnopharmacol. 2006 Sep 19;107(2):254-8. [Content Brief]
[2]. Li Q, et, al. Terpene Lactucopicrin Limits Macrophage Foam Cell Formation by a Reduction of Lectin-Like Oxidized Low-Density Lipoprotein Receptor-1 in Lipid Rafts. Mol Nutr Food Res. 2022 Feb;66(4):e2100905. [Content Brief]
[3]. He L, et al. Lactupicrin Inhibits Cytoplasmic Dynein-Mediated NF-κB Activation in Inflammated Macrophages and Alleviates Atherogenesis in Apolipoprotein E-Deficient Mice. Mol Nutr Food Res. 2021 Feb;65(4):e2000989. [Content Brief]
[4]. Bischoff TA, et al. Antimalarial activity of lactucin and lactucopicrin: sesquiterpene lactones isolated from Cichorium intybus L. J Ethnopharmacol. 2004 Dec;95(2-3):455-7. [Content Brief]
[5]. Rollinger JM, et al. Application of the in combo screening approach for the discovery of non-alkaloid acetylcholinesterase inhibitors from Cichorium intybus. Curr Drug Discov Technol. 2005 Sep;2(3):185-93. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4365 mL | 12.1826 mL | 24.3653 mL | 60.9132 mL |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL | 12.1826 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4365 mL | 6.0913 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 4.0609 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2183 mL | 3.0457 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4365 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0304 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6091 mL |