Art. -Nr.: HY-N8290

Lactupicrin

(Synonyms: Lactucopicrin)

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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.

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Reinheit: 99.62%
CAS. Nr.: 65725-11-3
Formel: C₂₃H₂₂O₇
Molecular Weight:410.42

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lactupicrin Chemical Structure

CAS. Nr.: 65725-11-3

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle Cholinesterase (ChE) Isoform-spezifische Produkte anzeigen :

AChE
BChE

Alle Parasite Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Real Time qPCR^[2]

Cell Line:

low-grade inflammatory macrophages
Concentration:

0.25, 0.5, 1 μM
Incubation Time:

24 h
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.

Western Blot Analysis^[3]

Cell Line:

Bone marrow-derived macrophages (BMDMs).
Concentration:

10, 20, 40 μM
Incubation Time:

24 h
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.

Real Time qPCR^[3]

Cell Line:

Bone marrow-derived macrophages (BMDMs) cells.
Concentration:

10, 20, 40 μM
Incubation Time:

24 h
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.

In Vivo

Lactupicrin (15-30 mg/kg, i.p.) shows analgesic activities and sedative properties in mice^[1].
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.

Animal Model:

Male Albino Swiss mice, weighing 24-28 g^[1].
Dosage:

15, 30 mg/kg
Administration:

i.p.
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).

Animal Model:

ApoE^-/- mice (C57BL/6), 8 weeks old, male, were fed with a high-fat diet (21% milk fat, 0.15% cholesterol)^[2].
Dosage:

1.2, 12, 120 mg/kg
Administration:

p.o., daily, 12 weeks
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.

Animal Model:

Male ApoE^-/- mice (C57BL/6), 6-8 weeks old, were fed a high fat diet (21% milk fat, 0.15% cholesterol)^[3].
Dosage:

12, 120 mg/kg
Administration:

p.o., daily, 12 weeks
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.

Chemical Information

CAS. Nr. 65725-11-3
Appearance Solid
Molecular Weight 410.42
Formel C₂₃H₂₂O₇
Color White to off-white
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
Synonyms

Lactucopicrin
Structure Classification
- Terpenoids
- Sesquiterpenes
- Phenols
- Monophenols
Initial Source
- Plants
- Compositae
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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Lactupicrin

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Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle Cholinesterase (ChE) Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lactupicrin Related Classifications

HY-N8290 Related Classifications