| CAS NO: | 137234-62-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| Molecular Weight (MW) | 349.31 |
|---|---|
| Formula | C16H14F3N5O |
| CAS No. | 137234-62-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 70 mg/mL (200.4 mM) |
| Water: <1 mg/mL | |
| Ethanol: 20 mg/mL (57.3 mM) | |
| Solubility (In vivo) | 30% PEG400+0.5% Tween80+5% propylene glycol: 10mg/mL |
| Synonyms | UK-109496; UK 109496; Voriconazole; UK109496; UK109,496; UK-109,496; UK 109,496; Vfend Chemical Name: (2R,3S)-2-(2,4-Difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol InChi Key: BCEHBSKCWLPMDN-MGPLVRAMSA-N InChi Code: InChI=1S/C16H14F3N5O/c1-10(15-14(19)5-20-7-22-15)16(25,6-24-9-21-8-23-24)12-3-2-11(17)4-13(12)18/h2-5,7-10,25H,6H2,1H3/t10-,16+/m0/s1 SMILES Code: C[C@@H](C1=NC=NC=C1F)[C@@](O)(C2=CC=C(F)C=C2F)CN3N=CN=C3 |
| In Vitro | In vitro activity: Voriconazole is active against certain opportunistic filamentous and dimorphic fungi (molds) and yeasts. Voriconazole in vitro activities are higher than or similar to those of itraconazole and amphotericin B for most of the molds tested, with the exceptions of R. arrhizus and S. schenckii. Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates Cell Assay: Voriconazole(UK-109496) is a second-generation triazole antifungal used to treat serious fungal infections. IC50 Value: Target: Antifungal Voriconazole displays potent activity against Candida, Cryptococcus and Aspergillus species. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes. |
|---|---|
| In Vivo | Voriconazole is significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised guinea pig with pulmonary aspergillosis. Voriconazole also has been shown to be effective in guinea pigs with experimental pulmonary or intracranial infections caused by C. neoformans. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) significantly reduces the colony counts in the tissues of selected Guinea pigs compared with those in the tissues of the controls. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) also results in reductions in colony counts in tissues compared with those in the tissues of Guinea pigs treated with caspofungin acetate (the difference is not statistically significant) and improves the survival times but does not sterilize tissues. Voriconazole (5 mg/kg/day, i.p.) combined with caspofungin acetate (CAS) at either dose reduces colony counts in tissues 1,000-fold over those for the controls and are the only regimens that significantly reduces the numbers of positive cultures. |
| Animal model | Guinea pig |
| Formulation & Dosage | 1.25, 5 mg/kg/day, i.p. |
| References | J Clin Microbiol. 1998 Jan;36(1):198-202; J Clin Microbiol. 2003 Aug;41(8):3623-6; Antimicrob Agents Chemother. 2002 Aug;46(8):2564-8. |
m.cnreagent.com