用途及描述：

科研试剂，广泛应用于分子生物学，药理学等科研方面。伊曲康唑的广谱抗菌活性与给药方式无关，它是通过抑制真菌细胞膜的必需成分-麦角固醇的合成而抑制真菌生长的。正常情况下，麦角固醇的前体羊毛甾醇在真菌细胞色素 Ｐ450催化下，进行14 －去甲基代谢。伊曲康唑在基底结合部和真菌 CYP交互作用，阻断其去甲基作用，使羊毛甾醇、14 －甲基甾醇蓄积在细胞膜上。麦角固醇合成受损导致真菌细胞膜的通透性改变，致使其细胞膜上酶的活性和壳多糖合成受阻。溶解性：在二氯甲烷中易溶，在四氢呋喃中略溶，溶于氯仿(50 mg/ml)，DMF (~0.5 mg/ml)，DMSO (50 mM)、水( 1 mg/ml，25℃)、甲醇或乙醇(10 mM,加热)中几乎不溶

储存条件：2 - 8 C，避光防潮密闭干燥。

伊曲康唑适用于治疗以下疾病：

1，用于全身性真菌感染，如曲霉病、念珠菌病、隐球菌病(包括隐球菌性脑膜炎)、组织胞浆菌病、孢子丝菌病、巴西副球孢子菌病、芽生菌病和其他多种少见的全身性或热带真菌病。

2，用于口腔、咽部(国外资料)、食管(国外资料)、外阴阴道念珠菌感染，以及真菌性结膜炎、真菌性角膜炎。

3，用于浅部真菌感染，如手足癣、体癣、股癣、花斑癣等。

4，用于皮肤癣菌和(或)酵母菌所致甲真菌病。

~assay98% (TLC)color whitesolubility chloroform: soluble50 mg/mL, clear, colorlessMode of action enzyme | inhibitsantibiotic activity spectrum fungistorage temp. 2-8 C

ApplicationItraconazole is a triazole antifungal agent. It is used to inhibit cytochrome P-450-dependent enzymes and ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis, and aspergillosis. It s different formulations are used to study Candida strains in murine invasive infections[1]. It has been used to study proliferative changes of the forestomach mucosa in alloxan-induced diabetic rats[2].

Biochem/physiol ActionsItraconazole inhibits cytochrome P-450-dependent enzymes which results in the inhibition of ergosterol synthesis. It does so by interacting with 14- demethylase, which is a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. Ergosterol is a crucial compenent of fungal cell membranes. Therefore, it s inhibition results in increased cellular permeability causing leakage of cellular contents. Itraconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and phospholipid biosynthesis.