| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Laninamivir Octanoate Monohydrate (Inavir, R-125489, CS-8958), the monohydrate form of Laninamivir Octanoate, is a long-acting neuraminidase inhibitor and a prodrug that has to be converted to the active form Laninamivir.
| ln Vitro |
Laninavir octanoate (CS-8958) has bactericidal action against H1N1 virus strains, H3N2 virus strains, and H2N2 (A/Singapore/1/57) virus strains, with IC50s of 631-1170 nM, 39.2-221 nM and 128 respectively[1].
|
|---|---|
| ln Vivo |
In an infection model, laninamivir octanoate (CS-8958; 95 μg/kg; intranasal administration; 3 times) given 4 hours before, 4 hours after, and 17 hours after infection significantly extended life [1].
|
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse (5-6 weeks old) infected with influenza A virus A/PR/8/34[1]
Doses: 0.2μmol/kg (95μg/kg) Route of Administration: intranasal administration Medicine; three doses; 4 hrs (hrs (hours)) before infection, 4 hrs (hrs (hours)) and 17 hrs (hrs (hours)) after infection. Experimental Results: demonstrated life-prolonging effect in infection model. |
| References |
[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.
[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. |
| Molecular Formula |
C21H38N4O9
|
|---|---|
| Molecular Weight |
490.547826290131
|
| Exact Mass |
490.264
|
| CAS # |
1233643-88-3
|
| Related CAS # |
Laninamivir;203120-17-6;Laninamivir octanoate;203120-46-1
|
| PubChem CID |
46919879
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.956
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
34
|
| Complexity |
723
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
[C@@H]1([C@H](OC)[C@H](O)COC(=O)CCCCCCC)OC(C(O)=O)=C[C@H](/N=C(\N)/N)[C@H]1NC(=O)C.[H]O[H]
|
| InChi Key |
IBFFAVWCRFPPNZ-QZAMVOJNSA-N
|
| InChi Code |
InChI=1S/C21H36N4O8.H2O/c1-4-5-6-7-8-9-16(28)32-11-14(27)18(31-3)19-17(24-12(2)26)13(25-21(22)23)10-15(33-19)20(29)30/h10,13-14,17-19,27H,4-9,11H2,1-3H3,(H,24,26)(H,29,30)(H4,22,23,25)1H2/t13-,14+,17+,18+,19+/m0./s1
|
| Chemical Name |
(2R,3R,4S)-3-acetamido-4-guanidino-2-((1R,2R)-2-hydroxy-1-methoxy-3-(octanoyloxy)propyl)-3,4-dihydro-2H-pyran-6-carboxylic
acid hydrate
|
| Synonyms |
CS-8958 CS 8958
R 125489R-125489R125489 CS8958 Inavir
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0385 mL | 10.1926 mL | 20.3853 mL | |
| 5 mM | 0.4077 mL | 2.0385 mL | 4.0771 mL | |
| 10 mM | 0.2039 mL | 1.0193 mL | 2.0385 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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