Efinaconazole (Synonyms: 艾氟康唑; KP-103)
目录号: PL14617 纯度: ≥99%
CAS No. :164650-44-6
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中文名称
Efinaconazole
中文别名
艾氟康唑(API);4-甲氧基-2-氟苯硼酸;艾菲康唑;艾菲康唑-D8;艾氟康唑;艾氟康唑API;艾菲康唑及杂质;艾菲康唑及相关杂质;(2R,3R)-2-(2,4-二氟苯基)-3-(4-亚甲基哌啶基-1-基)-1-(1H-1,2,4-三唑-1-基)丁烷-2-醇;(2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylidenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)butan-2-ol
英文名称
Efinaconazole
英文别名
KP-103;Efinaconazole [INN];UNII-J82SB7FXWB;SureCN300738;AC1LAJ21;Efinaconazole [USAN:INN];CHEMBL2103877;(2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol;KP 103;USAN;(αR,βR)-, α-(2,4-Difluorophenyl)-β-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidineethanol;(alphaR,betaR)-alpha-(2,4-Difluorophenyl)-beta-methyl-4-methylene-alpha-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidineethanol;KP 103 (pharmaceutical);Jublia;Efinaconazole;Efinaconazole(KP 103);(R,R)-2-(2,4-Difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)-2-butanol;(2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)-2-butanol;(2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylidenepiperidin-1-yl)-1-(1,2,4-triazol-1-yl)butan-2-ol;J82SB7FXWB;KP103;efinaconazolum;efinaconazol;Clenafin (TN);AK315814;Jublia (TN);Efinaconazole (JAN/USAN/INN);C18;1-Piperidineethanol, alpha-(2,4-difluorophenyl)-beta-methyl-4-methylene-alpha-(1H-1,2,4-triazol-1-ylmethyl)-, (alphaR,betaR)-;Ju
Cas No.
164650-44-6
分子式
C18H22F2N4O
分子量
348.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Efinaconazole (KP-103) 是一种三唑类抗真菌剂,以 MIC 值分别为 0.0039 μg/mL 和 0.00098 μg/mL 抑制 T. mentagrophytes SM-110 和 C. albicans ATCC 10231 菌株。Efinaconazole 对真菌病原体 (包括皮肤癣菌,念珠菌和马拉色菌属) 具有有效的体外活性。
生物活性
Efinaconazole (KP-103) is a triazole antifungal agent and againsts T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 μg/mL and 0.00098 μg/mL, respectively. Efinaconazole has a potent in vitro activity against fungal pathogens including dermatophytes, Candida and Malassezia species.
性状
Solid
IC50 & Target[1][2]
Fungal
体内研究(In Vivo)
Topical Efinaconazole solution (0.25 to 1%) is dose-dependently effective in treating both dermatophytoses, for 10 guinea pigs with interdigital tinea pedis or tinea corporis is investigated. The follow up study performs on day-30 and day-9 posttreatment demonstrated that the relapse rates for 1% Efinaconazole-treated animals with tinea pedis and for those with tinea corporis are 20 and 30%, respectively. When a single dose of 1% Efinaconazole is applied to the back skin 48 hours before fungal inoculation, 9 of the 10 animals are protected from the dermatophytosis, suggesting that active Efinaconazole is retained in skin tissue for at least 48 hours after dosing. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Tatsumi Y, et al. Mechanism of action of efinaconazole, a novel triazole antifungal agent. Antimicrob Agents Chemother. 2013 May;57(5):2405-9.
[2]. Tatsum Y, et al. KP-103, a novel triazole derivative, is effective in preventing relapse and successfully treating experimental interdigital tinea pedis and tinea corporis in guinea pigs. Microbiol Immunol. 2002;46(7):425-32.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (287.03 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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