Selamectin
Based on 1 Customer Validation
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.31%
- CAS. Nr.: 220119-17-5
- Formel: C43H63NO11
- Molecular Weight:769.96
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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- Reinheit & Dokumentation
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Biologische Aktivität
The transport of radiolabelled Selamectin through Caco-2 monolayers shows that Selamectin is P-glycoprotein (P-gp) substrates with a secretory/absorptive ratio of 4.7. Selamectin inhibits the efflux of Rh-123 from peripheral blood lymphocytes (PBL) and the concentration of inhibition is similar to that of Verapamil[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 220119-17-5
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Appearance Solid
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Molecular Weight 769.96
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Formel C43H63NO11
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Color White to off-white
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SMILES
O[C@@]12[C@@]3([H])/C(C(C)=C[C@@]1([H])C(O[C@]4([H])C[C@]5(O[C@@](C/C=C(C)/[C@@H](O[C@@]6([H])C[C@@H]([C@@H](O)[C@H](C)O6)OC)[C@@H](C)/C=C/C=C2\CO3)([H])C4)O[C@H](C7CCCCC7)[C@@H](C)CC5)=O)=N\O
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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
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (129.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (3.25 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 (3.25 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.
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
The cats are weighed on Days-2, 29 and 58 to calculate the dosing. Cats in group 1 (control group) remain untreated. On Day 0, the cats in group 3 are treated with fluralaner at the minimum recommending label dose of 40.0 mg per kg body weight. On Days 0, 30 and 60, the cats in group 2 are treated with the new spot-on formulation at the minimum recommending label dose of 1.0 mg/kg sarolaner and 6.0 mg/kg Selamectin. The cats are observed at different time points after treatment for possible adverse reactions to treatment. On Day 0, administration site observations are performed on all cats 30 min (±5 min), 3 h (±15 min) and 24 h (±1 h) and again on Days 3 and 5 after treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (291 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)
Verweise
[1]. Patsharaporn T Sarasombath, et al. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019 Apr;118(4):1289-1297. [Content Brief]
[2]. J Griffin, et al. Selamectin is a potent substrate and inhibitor of human and canine P-glycoprotein. J Vet Pharmacol Ther. 2005 Jun;28(3):257-65. [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 | 1.2988 mL | 6.4938 mL | 12.9877 mL | 32.4692 mL |
| 5 mM | 0.2598 mL | 1.2988 mL | 2.5975 mL | 6.4938 mL | |
| 10 mM | 0.1299 mL | 0.6494 mL | 1.2988 mL | 3.2469 mL | |
| 15 mM | 0.0866 mL | 0.4329 mL | 0.8658 mL | 2.1646 mL | |
| 20 mM | 0.0649 mL | 0.3247 mL | 0.6494 mL | 1.6235 mL | |
| 25 mM | 0.0520 mL | 0.2598 mL | 0.5195 mL | 1.2988 mL | |
| 30 mM | 0.0433 mL | 0.2165 mL | 0.4329 mL | 1.0823 mL | |
| 40 mM | 0.0325 mL | 0.1623 mL | 0.3247 mL | 0.8117 mL | |
| 50 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6494 mL | |
| 60 mM | 0.0216 mL | 0.1082 mL | 0.2165 mL | 0.5412 mL | |
| 80 mM | 0.0162 mL | 0.0812 mL | 0.1623 mL | 0.4059 mL | |
| 100 mM | 0.0130 mL | 0.0649 mL | 0.1299 mL | 0.3247 mL |
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