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1198769-38-8

中文名稱 化合物 T23174
英文名稱 Posaconazole (hydrate)
CAS 1198769-38-8
分子式 C37H44F2N8O5
分子量 718.81
MOL 文件 1198769-38-8.mol
1198769-38-8 結(jié)構(gòu)式 1198769-38-8 結(jié)構(gòu)式

基本信息

中文別名
泊沙康唑水合物
化合物 T23174
POSACONAZOLE水合物
英文別名
SCH-56592 HYDRATE
Posaconazole (hydrate)
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)粉末

常見問題列表

生物活性
Posaconazole水合物是Lanosterol-14去甲基酶抑制劑,IC50為0.25 nM。
靶點

antifungal

體外研究

Posaconazole has potent trypanocidal activity. Amiodarone acts synergistically with Posaconazole. Posaconazole also affects and disrupts Ca 2+ homeostasis in T. cruzi . Posaconazole blocks the biosynthesis of ergosterol, which is essential for parasite survival. Posaconazole has a clear, dose-dependent effect on proliferation of the epimastigote (extracellular) stages, with a minimal inhibitory concentration of 20 nM and an IC 50 of 14 nM. Against the clinically relevant intracellular amastigote form of the parasite, Posaconazole is even more potent. Posaconazole has the minimal inhibitory concentration and IC 50 values of 3 nM and 0.25 nM. Posaconazole is active against isolates of Candida and Aspergillus spp. that exhibit resistance to Fluconazole, Voriconazole, and Amphotericin B and is much more active than the other triazoles against zygomycetes.

體內(nèi)研究

Treatment of infected animals with amiodarone alone reduces parasitemia, increases survival 60 days pi (0% for untreated controls vs 40% for amiodarone-treated animals) and, when given in combination with Posaconazole, delays the development of parasitemia. Coadministration of Posaconazole and Boost Plus increases drug exposure compared to the administration of Posaconazole alone in the fasted state. Food, particularly meals high in fat content, significantly increases Posaconazole bioavailability. Systemic exposure to Posaconazole increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively. Posaconazole and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect. At twice-daily doses of ≥ 15 mg/kg of body weight, Posaconazole prolongs the survival of the mice and reduces tissue burden.

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