eraMivir
Peramivir trihydrate
CAS: 1041434-82-5
Molecular Formula: C15H30N4O5
eraMivir - Names and Identifiers
eraMivir - Physico-chemical Properties
| Molecular Formula | C15H30N4O5 |
| Molar Mass | 346.4225 |
| Solubility | DMSO 0.2 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| MDL | MFCD22417093 |
| In vivo study | Peramivir protected mice against infection with highly pathogenic avian influenza, and multiple-dose treatment was effective in ferrets. The performance of Peramivir in combination with Oseltamivir was better than that of each compound alone in the treatment of influenza infection in mice. Peramivir(30 mg/kg) can effectively promote the survival of mice infected with systemic replication H5N1 virus. Peramivir was protective in 30% of H1N1 virus mice at a dose of 0.5 mg/kg/day. But ineffective at lower doses when used as monotherapy. The combination of Peramivir and favipiravir can increase the cell survival rate, Peramivir at 0.025 mg/kg/day, 0.05 mg/kg/day, A dose of 0.1 mg/kg/day and a combination of 40 mg/kg/day Favipiravir increased cell survival by 10-50%. The combination of Peramivir and favipiravir resulted in increased lifespan, improved body weight and pulmonary hemorrhage scores and significant reductions in lung weight in H1N1-infected mice (1 mg/kg/day). And Rimantadine (5 mg/kg/day to 10 mg/kg/day) resulted in body weight loss of 1.69 and 0.69, respectively, whereas in A mouse model of sublethal influenza A(H3N2) virus, peramivir (3 mg/kg/day) and Rimantadine (10 mg/kg/day to 30 mg/kg/day) did not show any weight loss. |
eraMivir - Reference Information
| Overview | Paramivir itself is a cyclopentane derivative neuraminidase inhibitor. The drug can effectively inhibit the replication and spread of various influenza virus strains, and has the advantages of good tolerance, low toxicity, and practical injection. It is a promising anti-influenza drug. |
| antiviral activity | the antiviral activity of peramivir against laboratory virus strains and clinically isolated virus strains was investigated in cell culture tests. The EC50 value for seasonal influenza A H1N1 strains was 1 μM(0.09~21 μM,n = 5), 0.07 μM(<0.01~0.16 μM,n = 12) for influenza A H3N2 strains, and 2.2 μM(0.06~3.2 μM,n = 5) for influenza B strains. The relationship between antiviral activity, neuraminidase inhibitory activity in cell culture and persistent influenza virus replication in humans has not been established. Limited biochemical analysis, cell culture and animal model data show that the antiviral activity of peramivir and oseltamivir has a synergistic effect. There is no data to show that there is a synergy between peramivir and zanamivir. In the murine influenza A virus infection model, the combination of peramivir and oseltamivir showed enhanced antiviral activity, but its clinical significance is not clear. |
| Pharmacological mechanism | Paramivir is a cyclopentane anti-influenza virus drug that can bind to the active site of influenza virus neuraminidase and has inhibitory activity against human influenza A and B viruses. Biochemical analysis showed that peramivira could inhibit neuraminidase activity of several influenza A and B strains, and the median IC50 value for influenza A strains was 0.2nM(0.09~1.4nM,n = 15), and the median IC50 value for influenza B strains was 1.3nM(0.06 ~ 11nM,n = 8), the IC50 value for 2009H1N1A influenza virus strain (swine flu) ranges from 0.06 to 0.26nM. |
| Use | Paramivir itself is a cyclopentane derivative neuraminidase inhibitor. The drug can effectively inhibit the replication and spread of various influenza virus strains, and has the advantages of good tolerance, low toxicity, and practical injection. It is a promising anti-influenza drug. |
| biological activity | Peramivir Trihydrate (BCX-1812, RWJ-270201, S-021812) is a trihydrate Peramivir by anti-infective agents, which is a transition state simulation and a powerful influenza virus neuraminidase specific inhibitor with a median IC50 of 0.09 nM. |
Last Update：2024-04-09 21:01:54
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