Artemotil
Based on 1 publication(s) in Google Scholar
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.91%
- CAS. Nr.: 75887-54-6
- Formel: C17H28O5
- Molecular Weight:312.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Artemotil
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Biologische Aktivität
Beschreibung
IC50 & Target
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Plasmodium |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Ehrlich | IC50 |
13.1 μM
Compound: 4
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Cytotoxicity against mouse EAC after 3 days by MTT assay
Cytotoxicity against mouse EAC after 3 days by MTT assay
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[PMID: 8350087] |
| HUVEC | IC50 |
>50 μM
Compound: 13
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Inhibitory activity against human umbilical vein endothelial cells (HUVEC) was assayed using MTT colorimetric proliferation assay
Inhibitory activity against human umbilical vein endothelial cells (HUVEC) was assayed using MTT colorimetric proliferation assay
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[PMID: 14552753] |
| Vero | CC50 |
136057 nM
Compound: Arteether
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Cytotoxicity against african green monkey Vero C1008 cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero C1008 cells after 72 hrs by MTT assay
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[PMID: 23270565] |
In Vitro
The antimalarial activity of Artemotil is test in vitro against chloroquine-resistant and chloroquine-sensitive Plasmodium falciparum parasites. The mean 50% inhibitory concentration (IC50) for Artemotil is 1.61 nM (range 1.57-1.92 nM). Artemotil is approximately 2.5-fold more potent than artemisinin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley male rats (220-280 g)[2]
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Dosage:25 mg/kg; 1 mL/kg body weight
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Administration:Intravenous injection; daily; for 7 days
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Result:Anorectic toxicity was observed, and that caused significant reductions in food consumption and body weight after day 2.
Chemical Information
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CAS. Nr. 75887-54-6
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Appearance Solid
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Molecular Weight 312.40
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Formel C17H28O5
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Color White to off-white
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SMILES
C[C@@H]1[C@@](CC[C@@H](C)[C@]2([H])CC[C@]3(C)O4)([H])[C@@]2(OO3)[C@]4([H])O[C@@H]1OCC
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Synonyms
β-Arteether; (+)-Arteether; Arteether
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Structure Classification
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Inflammation
2024 Nov 28. PMID: 39607628
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (160.05 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (6.66 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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:
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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.
Protokoll
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Neurotoxicity Study
This protocol assesses in vitro neurotoxicity by combining neuronal viability, mitochondrial/metabolic activity, neurite outgrowth, and optional neuronal network function readouts. Calcein-AM or resazurin/PrestoBlue readouts estimate viable or metabolically active cells; βIII-tubulin immunofluorescence detects neuronal morphology and neurite networks; TMRE detects mitochondrial membrane potential; and MEA recordings detect functional changes in neuronal network activity.
Reinheit & Dokumentation
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Data Sheet (291 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Shmuklarsky MJ, et al. Comparison of beta-artemether and beta-arteether against malaria parasites in vitro and in vivo. Am J Trop Med Hyg. 1993 Mar;48(3):377-84. [Content Brief]
[2]. Li QG, et al. Arteether toxicokinetics and pharmacokinetics in rats after 25 mg/kg/day single and multiple doses. Eur J Drug Metab Pharmacokinet. 1999 Jul-Sep;24(3):213-23. [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 |
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| DMSO | 1 mM | 3.2010 mL | 16.0051 mL | 32.0102 mL | 80.0256 mL |
| 5 mM | 0.6402 mL | 3.2010 mL | 6.4020 mL | 16.0051 mL | |
| 10 mM | 0.3201 mL | 1.6005 mL | 3.2010 mL | 8.0026 mL | |
| 15 mM | 0.2134 mL | 1.0670 mL | 2.1340 mL | 5.3350 mL | |
| 20 mM | 0.1601 mL | 0.8003 mL | 1.6005 mL | 4.0013 mL | |
| 25 mM | 0.1280 mL | 0.6402 mL | 1.2804 mL | 3.2010 mL | |
| 30 mM | 0.1067 mL | 0.5335 mL | 1.0670 mL | 2.6675 mL | |
| 40 mM | 0.0800 mL | 0.4001 mL | 0.8003 mL | 2.0006 mL | |
| 50 mM | 0.0640 mL | 0.3201 mL | 0.6402 mL | 1.6005 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4001 mL | 1.0003 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3201 mL | 0.8003 mL |
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