1. Anti-infection
  2. Parasite
  3. Antimalarial agent 38

Antimalarial agent 38 is an orally active antimalarial agent, which inhibits Plasmodium falciparum D6 strain, Chloroquine (HY-17589A)-sensitive Thai strain and Chloroquine-resistant FcB1 strain and K1 strain, with IC50s of 0.5, 13, 1 and 13 μM, respectively. Antimalarial agent 38 is non-cytotoxic for mammalian cells MCR58 (IC50 >140 μM). Antimalarial agent 38 improves the survival rate of Plasmodium yoelii nigeriensis infected mouse model.

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Antimalarial agent 38

Antimalarial agent 38 Chemical Structure

CAS No. : 123580-46-1

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Description

Antimalarial agent 38 is an orally active antimalarial agent, which inhibits Plasmodium falciparum D6 strain, Chloroquine (HY-17589A)-sensitive Thai strain and Chloroquine-resistant FcB1 strain and K1 strain, with IC50s of 0.5, 13, 1 and 13 μM, respectively. Antimalarial agent 38 is non-cytotoxic for mammalian cells MCR58 (IC50 >140 μM). Antimalarial agent 38 improves the survival rate of Plasmodium yoelii nigeriensis infected mouse model[1].

Cellular Effect
Cell Line Type Value Description References
K562 IC50
> 20 μM
Compound: 29
Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion
Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion
[PMID: 9986718]
MRC5 IC50
> 70 μM
Compound: 1
Cytotoxicity against MRC5 cells
Cytotoxicity against MRC5 cells
[PMID: 17166718]
In Vivo

Antimalarial agent 38 (Compound 1) (10-50 mg/kg; p.o; daily; 4 days) shows active in Plasmodium yoelii nigeriensis infected mice[1].

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

Animal Model: Plasmodium yoelii nigeriensis N67 infected mice [1]
Dosage: 10 mg/kg, 50 mg/kg
Administration: p.o; daily; 4 days
Result: Showed dose-dependent reduction of parasitemia (around 40% of parasite growth inhibition at 50 mg/kg/day).
Molecular Weight

692.71

Formula

C36H40N2O12

CAS No.
Appearance

Solid

SMILES

O=C(COC1=C(OC)C=CC(C(OC2=C3C(O)=CC(OCC(N4CCN(CC4)CC5=CC=C(C(OC)=C5OC)OC)=O)=C2)=CC3=O)=C1)OCC

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 : 100 mg/mL (144.36 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 1.4436 mL 7.2180 mL 14.4361 mL
5 mM 0.2887 mL 1.4436 mL 2.8872 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

  • Dilution Calculator

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: ≥ 2.5 mg/mL (3.61 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (3.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (protect from light)

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
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 1.4436 mL 7.2180 mL 14.4361 mL 36.0901 mL
5 mM 0.2887 mL 1.4436 mL 2.8872 mL 7.2180 mL
10 mM 0.1444 mL 0.7218 mL 1.4436 mL 3.6090 mL
15 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4060 mL
20 mM 0.0722 mL 0.3609 mL 0.7218 mL 1.8045 mL
25 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4436 mL
30 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2030 mL
40 mM 0.0361 mL 0.1805 mL 0.3609 mL 0.9023 mL
50 mM 0.0289 mL 0.1444 mL 0.2887 mL 0.7218 mL
60 mM 0.0241 mL 0.1203 mL 0.2406 mL 0.6015 mL
80 mM 0.0180 mL 0.0902 mL 0.1805 mL 0.4511 mL
100 mM 0.0144 mL 0.0722 mL 0.1444 mL 0.3609 mL
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Antimalarial agent 38 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.

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Antimalarial agent 38
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