2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Anti-infection
  3. Dihydroorotate Dehydrogenase DNA/RNA Synthesis Parasite
  4. Lapachol

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity.

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

Lapachol Chemical Structure

Lapachol Chemical Structure

CAS No. : 84-79-7

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Lapachol:

Lapachol Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Lapachol

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View All Isoforms
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity[1][2][3].

IC50 & Target

Plasmodium

 

Leishmania

 

In Vitro

Lapachol (10, 30, 100 μM; 4 days) inhibits lymphocyte proliferation through inhibition of pyrimidine biosynthesis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lapachol Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Murine CD4 T cells
Concentration: 10, 30, 100 μM
Incubation Time: 4 days
Result: Inhibited the proliferation of murine CD4 T cells in a dose-dependent manner.
In Vivo

Lapachol (3 mg/kg and 10 mg/kg; orally; once a day for 4 weeks) reduces the severity of experimental arthritis in CIA mice models[1].
Lapachol (10 mg/kg; orally; once a day over 9 days) exhibits a remarkable reduction in leucocyte infiltration into the knee joint 6 h after mBSA challenge in male C57BL/6 mice (6 weeks old) with antigen-induced arthritis (AIA)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male DBA1/J mice (10-12 weeks old) with collagen-induced arthritis (CIA) models[1]
Dosage: 3 mg/kg and 10 mg/kg
Administration: Orally; once a day for 4 weeks
Result: Markedly attenuated the severity of arthritis in CIA mice at both doses.
Markedly reduced all histopathological features of arthritis severity.
Molecular Weight

242.27

Formula

C15H14O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(CC=C(C)C)=C1O)C2=CC=CC=C2C1=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (275.19 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 4.1276 mL 20.6381 mL 41.2763 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (10.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: 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 (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.06%

COA (249 KB) HNMR (237 KB) LCMS (95 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 (stored under nitrogen). 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 4.1276 mL 20.6381 mL 41.2763 mL 103.1907 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 mL 20.6381 mL
10 mM 0.4128 mL 2.0638 mL 4.1276 mL 10.3191 mL
15 mM 0.2752 mL 1.3759 mL 2.7518 mL 6.8794 mL
20 mM 0.2064 mL 1.0319 mL 2.0638 mL 5.1595 mL
25 mM 0.1651 mL 0.8255 mL 1.6511 mL 4.1276 mL
30 mM 0.1376 mL 0.6879 mL 1.3759 mL 3.4397 mL
40 mM 0.1032 mL 0.5160 mL 1.0319 mL 2.5798 mL
50 mM 0.0826 mL 0.4128 mL 0.8255 mL 2.0638 mL
60 mM 0.0688 mL 0.3440 mL 0.6879 mL 1.7198 mL
80 mM 0.0516 mL 0.2580 mL 0.5160 mL 1.2899 mL
100 mM 0.0413 mL 0.2064 mL 0.4128 mL 1.0319 mL
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Lapachol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lapachol84-79-7Dihydroorotate DehydrogenaseDNA/RNA SynthesisParasiteDHODHnaphthoquinoneimmunosuppressivelymphocytespyrimidine synthesisvitamin Kantitumorneoplastic cellsanti-LeishmaniaInhibitorinhibitorinhibit

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