Biochem/physiol Actions
Laninamivir (R-125489) prodrug with improved in vivo efficacy than R-125489 and Zanamivir in a mouse influenza virus A (IAV) infection model.
Laninamivir octanoate (CS-8958) is the prodrug form of Laninamivir (R-125489), a potent inhibitor agianst the neuraminidase (NA) activities of various type A and B influenza viruses, including subtypes N1 to N9 and Oseltamivir-resistant strains. When administered intranasally (3X 0.2 μmol/kg; 4 h before, 4 h & 18 h post infection), CS-8958 shows improved in vivo efficacy (100% survival rate on day 20 post infecfion) than R-125489 (100/30/20% survival rate on day 7/10/20 post infecfion) and Zanamivir (100%/0% death on day 7/10) in a mouse influenza virus A/Puerto Rico/8/34 infection model, with prolonged survival effect post a single dosage given even 7 days before infection. Note: Laninamivir octanoate is mainly used for in vivo studies, it exhibits only weak to little antiviral potency before it is converted to the active drug form.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | 2-8°C |
| SMILES string | CCCCCCCC(OC[C@@H](O)[C@@H](OC)[C@@]1([H])[C@H](NC(C)=O)[C@@H](NC(N)=N)C=C(C(O)=O)O1)=O |
| 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 |
| InChI key | UKTIJASCFRNWCB-RMIBSVFLSA-N |
