| 规格或纯度 | 10mM in DMSO |
|---|---|
| 英文名称 | Baloxavir marboxil |
| 英文别名 | Carbonic acid,[[(12aR)?-?12-?[(11S)?-?7,?8-?difluoro-?6,?11-?dihydrodibenzo[b,?e]?thiepin-?11-?yl]?-?3,?4,?6,?8,?12,?12a-?hexahydro-?6,?8-?dioxo-?1H-?[1,?4]?oxazino[3,?4-?c]?pyrido[2,?1-?f]?[1,?2,?4]?triazin-?7-?yl]?oxy]?methyl methyl ester |
| 生化机理 | Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug. |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Information Baloxavir marboxil Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug. In vivo Single-dose oral baloxavir marboxil is well tolerated, had a favorable safety profile, and has favorable pharmacokinetic characteristics, including a long half-life, supporting single oral dosing. In nonclinical studies, baloxavir marboxil is a prodrug and is converted to an active form, baloxavir acid, by hydrolysis. After single oral administration in rats and monkeys, plasma concentrations of baloxavir marboxil are below the lower limit of quantification (LLOQ) at all sampling points, and area under the plasma concentration-time curve of baloxavir acid increased dose proportionally. The major excretion route of radioactivity is via fecal excretion, whereas urinary excretion was low in rats and monkeys. Baloxavir marboxil has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents. In murine models of seasonal influenza and avian influenza A(H5N1) or A(H7N9), orally administered baloxavir is associated with rapid reductions in pulmonary viral loads and decreased mortality. Information Baloxavir marboxil Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug. In vivo Single-dose oral baloxavir marboxil is well tolerated, had a favorable safety profile, and has favorable pharmacokinetic characteristics, including a long half-life, supporting single oral dosing. In nonclinical studies, baloxavir marboxil is a prodrug and is converted to an active form, baloxavir acid, by hydrolysis. After single oral administration in rats and monkeys, plasma concentrations of baloxavir marboxil are below the lower limit of quantification (LLOQ) at all sampling points, and area under the plasma concentration-time curve of baloxavir acid increased dose proportionally. The major excretion route of radioactivity is via fecal excretion, whereas urinary excretion was low in rats and monkeys. Baloxavir marboxil has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents. In murine models of seasonal influenza and avian influenza A(H5N1) or A(H7N9), orally administered baloxavir is associated with rapid reductions in pulmonary viral loads and decreased mortality. |
| ALogP | 2.602 |
|---|---|
| Rotatable Bond | 6 |
| DMSO(mM) Max Solubility | 174.962820400665 |
| DMSO(mg / mL) Max Solubility | 100 |
| Water(mg / mL) Max Solubility | ＜1 |
| IUPAC Name | [(3R)-2-[(11S)-7,8-difluoro-6,11-dihydrobenzo[c][1]benzothiepin-11-yl]-9,12-dioxo-5-oxa-1,2,8-triazatricyclo[8.4.0.03,8]tetradeca-10,13-dien-11-yl]oxymethyl methyl carbonate |
|---|---|
| INCHI | InChI=1S/C27H23F2N3O7S/c1-36-27(35)39-14-38-25-19(33)8-9-31-24(25)26(34)30-10-11-37-12-21(30)32(31)23-15-6-7-18(28)22(29)17(15)13-40-20-5-3-2-4-16(20)23/h2-9,21,23H,10-14H2,1H3/t21-,23+/m1/s1 |
| InChi Key | RZVPBGBYGMDSBG-GGAORHGYSA-N |
| Canonical SMILES | COC(=O)OCOC1=C2C(=O)N3CCOCC3N(N2C=CC1=O)C4C5=C(CSC6=CC=CC=C46)C(=C(C=C5)F)F |
| 分子式 |
C27H23F2N3O7S |
| PubChem CID | 124081896 |
| 分子量 | 571.55 |
| 象形图 |
Environmental Hazard |
|---|---|
| 危险声明 |
H411: Toxic to aquatic life with long lasting effects |
| 预防措施声明 | P273,P501,P391 |
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