Didesethyl chloroquine
Based on 1 Customer Validation
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.
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- Purity: 99.62%
- CAS No.: 4298-14-0
- 화학식: C14H18ClN3
- 분자량:263.77
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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CAS No. 4298-14-0
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Appearance Solid
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분자량 263.77
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화학식 C14H18ClN3
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Color White to light yellow
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SMILES
CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN
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Synonyms
Bisdesethylchloroquine
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (269 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Essien EE, et al. Effects of chloroquine and didesethylchloroquine on rabbit myocardium and mitochondria. J Pharm Pharmacol. 1986;38(7):543-546. [Content Brief]
[2]. Biot C, et al. Synthesis and antimalarial activity in vitro of potential metabolites of ferrochloroquine and related compounds. Bioorg Med Chem. 1999;7(12):2843-2847. [Content Brief]
[3]. Kumar M, et al. Molecular docking studies of chloroquine and its derivatives against P23pro-zbd domain of chikungunya virus: Implication in designing of novel therapeutic strategies. J Cell Biochem. 2019;120(10):18298-18308. [Content Brief]
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 |
Didesethyl chloroquine Related Classifications
HY-100662 Related Classifications
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