| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
Laninamivir Octanoate (CS-8958, Inavir, R-125489) is a novel long-acting neuraminidase inhibitor that is a prodrug and has to be converted to the active form Laninamivir. Laninamivir inhibits avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2) with IC50s of 0.90 nM, 1.83 nM and 3.12 nM, respectively. It exhibits clinical efficacy for both treatment and prophylaxis of influenza virus infection, resulting from hydrolytic bioactivation into its pharmacologically active metabolite laninamivir in the pulmonary tissue.
| ln Vitro |
Laninamivir Octanoate (CS-8958) demonstrates inhibitory action against the H1N1 strain, H3N2 strain and H2N2 (A/Singapore/1/57) virus with IC50 of 631-1170 nM, 39.2-221 nM and 128 nM respectively. [1].
|
|---|---|
| ln Vivo |
Infection models demonstrated notable life-prolonging benefits when lanamivir octanoate (CS-8958; 95 μg/kg; intranasally; 3 doses; 4 hours before infection, 4 hours, and 17 hours after infection) was administered [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: 0.2 μmol/kg (95 μg/kg) Route of Administration: intranasal Administration; 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 |
|
| Additional Infomation |
Laninamivir octanoate hydrate is a fatty acid ester.
Laninamivir octanoate has been used in trials studying the treatment of Asthma. See also: Laninamivir octanoate monohydrate (annotation moved to). |
| Molecular Formula |
C21H36N4O8
|
|---|---|
| Molecular Weight |
472.5325
|
| Exact Mass |
472.253
|
| Elemental Analysis |
C, 53.38; H, 7.68; N, 11.86; O, 27.09
|
| CAS # |
203120-46-1
|
| Related CAS # |
Laninamivir;203120-17-6;Laninamivir octanoate hydrate;1233643-88-3
|
| PubChem CID |
9847629
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.572
|
| LogP |
1.54
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
33
|
| Complexity |
723
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
O1C(C(=O)O[H])=C([H])[C@@]([H])([C@]([H])([C@]1([H])[C@@]([H])([C@@]([H])(C([H])([H])OC(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)O[H])OC([H])([H])[H])N([H])C(C([H])([H])[H])=O)/N=C(\N([H])[H])/N([H])[H]
|
| InChi Key |
UKTIJASCFRNWCB-RMIBSVFLSA-N
|
| InChi Code |
InChI=1S/C21H36N4O8/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)/t13-,14+,17+,18+,19+/m0/s1
|
| Chemical Name |
(2R,3R,4S)-3-acetamido-4-(diaminomethylideneamino)-2-[(1R,2R)-2-hydroxy-1-methoxy-3-octanoyloxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid
|
| Synonyms |
Laninamivir Octanoate; CS-8958; CS 8958; CS8958; R-125489; R 125489; R125489;
|
| 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) |
DMSO : ~100 mg/mL (~211.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1163 mL | 10.5813 mL | 21.1627 mL | |
| 5 mM | 0.4233 mL | 2.1163 mL | 4.2325 mL | |
| 10 mM | 0.2116 mL | 1.0581 mL | 2.1163 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
