Moxidectin
Based on 1 publication(s) in Google Scholar
Moxidectin (CL301423) is an orally active and brain-penetrant macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk.
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- Pureza : 99.32%
- No. CAS: 113507-06-5
- Fòrmula: C37H53NO8
- Peso molecular:639.82
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Moxidectin
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Actividad biológica
Descripciòn
IC50 & Target
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Macrolide |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 113507-06-5
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Appearance Solid
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Peso molecular 639.82
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Fòrmula C37H53NO8
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Color White to off-white
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SMILES
C/C([C@H]([C@H](/C1=N/OC)C)O[C@]2(C1)C[C@](OC([C@@](C=C(C)[C@@H](O)[C@@]3([H])OC/C4=C\C=C\[C@H](C)C5)([H])[C@@]34O)=O)([H])C[C@](C/C=C5\C)([H])O2)=C\C(C)C
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Synonyms
CL301423
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (156.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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)
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: ≥ 2.5 mg/mL (3.91 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 (3.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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:
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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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (564 KB)
- English - EN (564 KB)
- Français - FR (564 KB)
- Deutsch - DE (564 KB)
- Norwegian - NO (564 KB)
- Español - ES (564 KB)
- Swedish - SV (564 KB)
- Italian - IT (564 KB)
- Korean - KR (564 KB)
- Portuguese - PT (564 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Moxidectin, From Wikipedia
[2]. Perez M, et al. In vitro and in vivo interaction of moxidectin with BCRP/ABCG2. Chem Biol Interact. 2009 Jun 15;180(1):106-12. [Content Brief]
[3]. Kiki-Mvouaka S, et al. Role of P-glycoprotein in the disposition of macrocyclic lactones: A comparison between ivermectin, eprinomectin, and moxidectin in mice. Drug Metab Dispos. 2010 Apr;38(4):573-80. [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 | 1 mM | 1.5629 mL | 7.8147 mL | 15.6294 mL | 39.0735 mL |
| 5 mM | 0.3126 mL | 1.5629 mL | 3.1259 mL | 7.8147 mL | |
| 10 mM | 0.1563 mL | 0.7815 mL | 1.5629 mL | 3.9073 mL | |
| 15 mM | 0.1042 mL | 0.5210 mL | 1.0420 mL | 2.6049 mL | |
| 20 mM | 0.0781 mL | 0.3907 mL | 0.7815 mL | 1.9537 mL | |
| 25 mM | 0.0625 mL | 0.3126 mL | 0.6252 mL | 1.5629 mL | |
| 30 mM | 0.0521 mL | 0.2605 mL | 0.5210 mL | 1.3024 mL | |
| 40 mM | 0.0391 mL | 0.1954 mL | 0.3907 mL | 0.9768 mL | |
| 50 mM | 0.0313 mL | 0.1563 mL | 0.3126 mL | 0.7815 mL | |
| 60 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6512 mL | |
| 80 mM | 0.0195 mL | 0.0977 mL | 0.1954 mL | 0.4884 mL | |
| 100 mM | 0.0156 mL | 0.0781 mL | 0.1563 mL | 0.3907 mL |
Moxidectin Related Classifications
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