2. Metabolic Enzyme/Protease NF-κB Neuronal Signaling Anti-infection
  3. LOX-1 NF-κB Cholinesterase (ChE) Parasite
  4. Lactupicrin

Lactupicrin  (Synonyms: Lactucopicrin)

Cat. No.: HY-N8290 Purity: 99.97%
Data Sheet
SDS
COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

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.

For research use only. We do not sell to patients.

Lactupicrin Chemical Structure

Lactupicrin Chemical Structure

CAS No. : 65725-11-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 405 In-stock
Solution
10 mM * 1 mL in DMSO USD 426 In-stock
Solid
5 mg USD 473 In-stock
10 mg USD 788 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2][3][4][5].

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.
Molecular Weight

410.42

Formula

C23H22O7
CAS No.
Appearance

Solid

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
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.97%

Data Sheet (285 KB) SDS (393 KB)

COA (257 KB) HNMR (287 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

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
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Lactupicrin Related Classifications

Keywords:

Lactupicrin65725-11-3LactucopicrinLOX-1NF-κBCholinesterase (ChE)ParasiteLectin-like oxidized low-density lipoprotein receptor-1Nuclear factor-κBNuclear factor-kappaBanalgesic activitysedative activityfoam cell formationatherosclerosisantimalarialAlzheimer’s diseaseInhibitorinhibitorinhibit

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