检测方案
≥98% (HPLC)
形式
powder
旋光性
[α]/D -24 to -32°, c = 1.0 in chloroform-d
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
InChI
1S/C37H42F2N8O4/c1-3-35(26(2)48)47-36(49)46(25-42-47)31-7-5-29(6-8-31)43-14-16-44(17-15-43)30-9-11-32(12-10-30)50-20-27-19-37(51-21-27,22-45-24-40-23-41-45)33-13-4-28(38)18-34(33)39/h4-13,18,23-27,35,48H,3,14-17,19-22H2,1-2H3/t26-,27+,35-,37-/m0/s1
InChI key
RAGOYPUPXAKGKH-XAKZXMRKSA-N
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应用
泊沙康唑用于：
- 土曲霉抗真菌药敏试验
- 作为羊毛甾醇14α-脱甲基酶 (CYP51) 特异性抑制剂，研究其对白色念珠菌细胞膜通透性的影响
- 研究其对前鞭毛体的影响
生化/生理作用
泊沙康唑是一种高效的广谱抗真菌剂，可抑制念珠菌引起的酵母菌感染。它通过抑制羊毛甾醇14α-脱甲基酶 (CYP51)阻断真菌生长。与其他抗真菌唑类药物相反，泊沙康唑据报道不会诱导外排泵机制。泊沙康唑对各类南美锥虫病的病原体克氏锥虫菌株具有抑制作用。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Galina I Lepesheva et al.
The Journal of biological chemistry, 285(33), 25582-25590 (2010-06-10)
Trypanosoma cruzi causes Chagas disease (American trypanosomiasis), which threatens the lives of millions of people and remains incurable in its chronic stage. The antifungal drug posaconazole that blocks sterol biosynthesis in the parasite is the only compound entering clinical trials
Israel Molina et al.
Current opinion in infectious diseases, 28(5), 397-407 (2015-07-24)
The current therapeutic scenario against Chagas disease has been recently updated with the use of the triazoles in clinical trials and several experimental assays (in-vitro and in-vivo models) which are bringing novel and promising evidence for the treatment of Chagas
Chiung-Kuang Chen et al.
PLoS neglected tropical diseases, 4(4), e651-e651 (2010-04-14)
Chagas Disease is the leading cause of heart failure in Latin America. Current drug therapy is limited by issues of both efficacy and severe side effects. Trypansoma cruzi, the protozoan agent of Chagas Disease, is closely related to two other
Harrys A Torres et al.
The Lancet. Infectious diseases, 5(12), 775-785 (2005-11-29)
Posaconazale is a new triazole drug being investigated in phase III clinical trials for the treatment and prevention of invasive fungal infections. In-vitro and in-vivo studies showed that posaconazole has broad-spectrum activity against most Candida species, Cryptococcus neoformans, Aspergillus species
Yanjun Li et al.
Clinical pharmacokinetics, 49(6), 379-396 (2010-05-21)
Posaconazole is a recently approved lipophilic triazole antifungal agent that exhibits potent and broad-spectrum antifungal activity in vitro and in vivo against most Candida spp., Cryptococcus neoformans, Aspergillus spp., many Zygomycetes, endemic fungi and dermatophytes. It has been documented that
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