164650-44-6
164650-44-6 structure
- Name: Efinaconazole
- Chemical Name: efinaconazole
- CAS Number: 164650-44-6
- Molecular Formula: C18H22F2N4O
- Molecular Weight: 348.390
- Catalog: API Synthetic anti-infective drugs Antifungal drugs
- Create Date: 2018-04-13 08:00:00
- Modify Date: 2024-01-02 16:50:51
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Efinaconazole(KP-103) is a novel triazole antifungal drug currently under development as a topical treatment for onychomycosis.IC50 value: 0.0039 ug/ml (MIC for T. mentagrophytes SM-110) [1]Target: antifungal agentin vitro: Efinaconazole was 4-fold more active than itraconazole against T. mentagrophytes SM-110 (MICs of 0.0039 and 0.016 μg/ml, respectively). Similarly, efinaconazole was 8-fold more active than clotrimazole against C. albicans ATCC 10231 (MICs of 0.00098 and 0.0078 μg/ml, respectively) [1]. In a comprehensive survey of 1,493 isolates, efinaconazole MICs against T. rubrum and T. mentagrophytes ranged from ≤ 0.002 to 0.06 μg/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 μg/ml, respectively. Efinaconazole MICs against 105 C. albicans isolates ranged from ≤ 0.0005 to >0.25 μg/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 μg/ml at 24 and 48 h, respectively [2].in vivo: The therapeutic efficacy of KP-103, a triazole derivative, for 10 guinea pigs with interdigital tinea pedis or tinea corporis was investigated. Topical KP-103 solution (0.25 to 1%) was dose-dependently effective in treating both dermatophytoses. A 1% KP-103-treatment rendered all infected skins culture-negative on day-2 posttreatment [3].
| Name | efinaconazole |
|---|---|
| Synonyms |
Efinaconazole [USAN:INN]
(2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol UNII-J82SB7FXWB KP-103 (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylidenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)butan-2-ol Efinaconazole (JAN/USAN/INN) Efinaconazole 1-Piperidineethanol, α-(2,4-difluorophenyl)-β-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-, (αR,βR)- Jublia Efinaconazole [INN] |
| Description | Efinaconazole(KP-103) is a novel triazole antifungal drug currently under development as a topical treatment for onychomycosis.IC50 value: 0.0039 ug/ml (MIC for T. mentagrophytes SM-110) [1]Target: antifungal agentin vitro: Efinaconazole was 4-fold more active than itraconazole against T. mentagrophytes SM-110 (MICs of 0.0039 and 0.016 μg/ml, respectively). Similarly, efinaconazole was 8-fold more active than clotrimazole against C. albicans ATCC 10231 (MICs of 0.00098 and 0.0078 μg/ml, respectively) [1]. In a comprehensive survey of 1,493 isolates, efinaconazole MICs against T. rubrum and T. mentagrophytes ranged from ≤ 0.002 to 0.06 μg/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 μg/ml, respectively. Efinaconazole MICs against 105 C. albicans isolates ranged from ≤ 0.0005 to >0.25 μg/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 μg/ml at 24 and 48 h, respectively [2].in vivo: The therapeutic efficacy of KP-103, a triazole derivative, for 10 guinea pigs with interdigital tinea pedis or tinea corporis was investigated. Topical KP-103 solution (0.25 to 1%) was dose-dependently effective in treating both dermatophytoses. A 1% KP-103-treatment rendered all infected skins culture-negative on day-2 posttreatment [3]. |
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| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 512.2±60.0 °C at 760 mmHg |
| Molecular Formula | C18H22F2N4O |
| Molecular Weight | 348.390 |
| Flash Point | 263.6±32.9 °C |
| Exact Mass | 348.176178 |
| PSA | 54.18000 |
| LogP | 3.46 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.590 |
| Storage condition | 2~8℃ |
| Hazard Codes | Xi |
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