Laninamivir octanoate
Based on 1 Customer Validation
Laninamivir octanoate (CS-8958), a proagent of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses.
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- Pureté: 98.57%
- CAS No.: 203120-46-1
- Formule: C21H36N4O8
- Masse moléculaire:472.53
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Laninamivir octanoate (CS-8958) shows inhibitory activity with an IC50 of 631-1170 nM, 39.2-221 nM and 128 nM to the H1N1 viruses strains, H3N2 viruses strains and H2N2 (A/Singapore/1/57) virus, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (5-6 weeks old) infected with influenza A virus A/PR/8/34[1]
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Dosage:0.2 μmol/kg (95 μg/kg)
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Administration:Intranasal administration; three dose; at 4 h before and 4 h and 17 h postinfection
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Result:Showed life-prolonging effect in infected model.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 203120-46-1
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Appearance Solid
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Masse moléculaire 472.53
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Formule C21H36N4O8
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Color White to off-white
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SMILES
CC(N[C@H]1[C@](OC(C(O)=O)=C[C@@H]1NC(N)=N)([H])[C@H](OC)[C@H](O)COC(CCCCCCC)=O)=O
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Synonyms
CS-8958
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (211.63 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.29 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.
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.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Makoto Yamashita, et al. CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity. Antimicrob Agents Chemother. 2009 Jan;53(1):186-92. [Content Brief]
[2]. Hideyuki Ikematsu, et al. Laninamivir octanoate: a new long-acting neuraminidase inhibitor for the treatment of influenza. Expert Rev Anti Infect Ther. 2011 Oct;9(10):851-7. [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 |
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| DMSO | 1 mM | 2.1163 mL | 10.5813 mL | 21.1627 mL | 52.9067 mL |
| 5 mM | 0.4233 mL | 2.1163 mL | 4.2325 mL | 10.5813 mL | |
| 10 mM | 0.2116 mL | 1.0581 mL | 2.1163 mL | 5.2907 mL | |
| 15 mM | 0.1411 mL | 0.7054 mL | 1.4108 mL | 3.5271 mL | |
| 20 mM | 0.1058 mL | 0.5291 mL | 1.0581 mL | 2.6453 mL | |
| 25 mM | 0.0847 mL | 0.4233 mL | 0.8465 mL | 2.1163 mL | |
| 30 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7636 mL | |
| 40 mM | 0.0529 mL | 0.2645 mL | 0.5291 mL | 1.3227 mL | |
| 50 mM | 0.0423 mL | 0.2116 mL | 0.4233 mL | 1.0581 mL | |
| 60 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8818 mL | |
| 80 mM | 0.0265 mL | 0.1323 mL | 0.2645 mL | 0.6613 mL | |
| 100 mM | 0.0212 mL | 0.1058 mL | 0.2116 mL | 0.5291 mL |
Laninamivir octanoate Related Classifications
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