Lumefantrine
Based on 2 publication(s) in Google Scholar
Lumefantrine is an active antimalarial molecule used in combination with Artemether as a first- and second-line antimalarial drug with oral activity.
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- Purity: 99.40%
- CAS No.: 82186-77-4
- 화학식: C30H32Cl3NO
- 분자량:528.94
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Lumefantrine
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Biological Activity
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Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>20 μM
Compound: LUM
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Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by neutral red dye based analysis
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by neutral red dye based analysis
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[PMID: 33666415] |
| Huh-7 | CC50 |
>10 μM
Compound: GNF-Pf-1971
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice[1]
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Dosage:8 mg/kg; daily; 3 days
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Administration:Parenteral administration
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Result:Kept parasite rate at 5% or below.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 82186-77-4
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Appearance Solid
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분자량 528.94
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화학식 C30H32Cl3NO
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Color Light yellow to yellow
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SMILES
OC(CN(CCCC)CCCC)C1=CC(Cl)=CC(/C2=C\C3=CC=C(Cl)C=C3)=C1C4=C2C=C(Cl)C=C4
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Synonyms
Benflumetol
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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 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Omega
2019 Jan 31;4(1):2353-2361. PMID: 30729228 -
용액&용해도
DMF : 25 mg/mL (47.26 mM; ultrasonic and warming and heat to 60°C)
DMSO : 2 mg/mL (3.78 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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% DMF 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.2 mg/mL (0.38 mM); Clear solution
This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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: 0.2 mg/mL (0.38 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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 (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yufan Ma, et al. Enhanced antimalarial activity by a novel artemether-lumefantrine lipid emulsion for parenteral administration. Antimicrob Agents Chemother. 2014 Oct;58(10):5658-65. [Content Brief]
[2]. Ndounga M, et al. Artesunate-amodiaquine versus artemether-lumefantrine for the treatment of acute uncomplicated malaria in Congolese children under 10 years old living in a suburban area: a randomized study. Malar J. 2015 Oct 29;14(1):423. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMF | 1 mM | 1.8906 mL | 9.4529 mL | 18.9057 mL | 47.2643 mL |
| DMF | 5 mM | 0.3781 mL | 1.8906 mL | 3.7811 mL | 9.4529 mL |
| 10 mM | 0.1891 mL | 0.9453 mL | 1.8906 mL | 4.7264 mL | |
| 15 mM | 0.1260 mL | 0.6302 mL | 1.2604 mL | 3.1510 mL | |
| 20 mM | 0.0945 mL | 0.4726 mL | 0.9453 mL | 2.3632 mL | |
| 25 mM | 0.0756 mL | 0.3781 mL | 0.7562 mL | 1.8906 mL | |
| 30 mM | 0.0630 mL | 0.3151 mL | 0.6302 mL | 1.5755 mL | |
| 40 mM | 0.0473 mL | 0.2363 mL | 0.4726 mL | 1.1816 mL |