1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. Didesethyl chloroquine

Didesethyl chloroquine  (Synonyms: Bisdesethylchloroquine)

Cat. No.: HY-100662 Purity: 98.57%
Handling Instructions Technical Support

Didesethyl chloroquine (Bisdesethylchloroquine) is the major metabolite of the antimalarial agent Chloroquine (HY-17589A). Didesethyl chloroquine is a potent myocardial inhibitor. Didesethyl chloroquine reduces calcium binding and accumulation in cardiac mitochondria, induces mitochondrial swelling, rupture and membrane conformational changes. Didesethyl chloroquine inhibits the growth of Plasmodium falciparum strains. Didesethyl chloroquine can be used in research related to malaria, chikungunya virus infection, and cardiovascular and cerebrovascular diseases.

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

Didesethyl chloroquine

Didesethyl chloroquine Chemical Structure

CAS No. : 4298-14-0

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1 mg In-stock
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Description

Didesethyl chloroquine (Bisdesethylchloroquine) is the major metabolite of the antimalarial agent Chloroquine (HY-17589A). Didesethyl chloroquine is a potent myocardial inhibitor. Didesethyl chloroquine reduces calcium binding and accumulation in cardiac mitochondria, induces mitochondrial swelling, rupture and membrane conformational changes. Didesethyl chloroquine inhibits the growth of Plasmodium falciparum strains. Didesethyl chloroquine can be used in research related to malaria, chikungunya virus infection, and cardiovascular and cerebrovascular diseases[1][2][3].

In Vitro

Didesethyl chloroquine significantly inhibits energy-independent calcium binding and energy-driven calcium accumulation in isolated rabbit heart mitochondria[1].
Didesethyl chloroquine binds to the P23pro-zbd domain of Chikungunya virus, with a LibDock score of 106.229, and interacts with the Ala1356, Asn1357 and Ala1401 residues[3].

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

Molecular Weight

263.77

Formula

C14H18ClN3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (379.12 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 3.7912 mL 18.9559 mL 37.9118 mL
5 mM 0.7582 mL 3.7912 mL 7.5824 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. 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 (9.48 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.48 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 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:

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).
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: 99.91%

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. 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 3.7912 mL 18.9559 mL 37.9118 mL 94.7795 mL
5 mM 0.7582 mL 3.7912 mL 7.5824 mL 18.9559 mL
10 mM 0.3791 mL 1.8956 mL 3.7912 mL 9.4780 mL
15 mM 0.2527 mL 1.2637 mL 2.5275 mL 6.3186 mL
20 mM 0.1896 mL 0.9478 mL 1.8956 mL 4.7390 mL
25 mM 0.1516 mL 0.7582 mL 1.5165 mL 3.7912 mL
30 mM 0.1264 mL 0.6319 mL 1.2637 mL 3.1593 mL
40 mM 0.0948 mL 0.4739 mL 0.9478 mL 2.3695 mL
50 mM 0.0758 mL 0.3791 mL 0.7582 mL 1.8956 mL
60 mM 0.0632 mL 0.3159 mL 0.6319 mL 1.5797 mL
80 mM 0.0474 mL 0.2369 mL 0.4739 mL 1.1847 mL
100 mM 0.0379 mL 0.1896 mL 0.3791 mL 0.9478 mL
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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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Product Name:
Didesethyl chloroquine
Cat. No.:
HY-100662
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