性能描述

溶解性：This product is soluble in a CHCl3:MeOH mixture(1:1, 25 mg/ml), with heat and sonication as needed,yielding a clear, colorless solution. It is also very slightly soluble in water, slightly soluble in alcohol, and sparingly soluble in chloroform and methylene chloride.2 This product is also soluble in DMSO(0.4 mg/ml).

Application

Econazole is a broad spectrum antimycotic similar to ketoconazole. It has some action against Gram positive bacteria. It is used topically in dermatomycoses as well as orally and parenterally. It is used for studies on processes such as platelet serotonin uptake, prostanoid biosynthesis, EDHF-mediated relaxation, and Ca2+ transport pathways in thymic lymphocytes.

Biochem/physiol Actions

Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. Inhibition of ergosterol results in increased cellular permeability causing leakage of cellular contents. Econazole 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. It Inhibits Ca2+ transport pathways in thymic lymphocytes.
 
用途：有抑制真菌作用，高浓度时也可具杀菌作用。该品可抑制麦角甾醇或其他甾醇类的生物合成，损伤真菌细胞膜和改变其通透性，以致重要的细胞内物质外漏；该品也可抑制真菌的甘油三酯和磷脂的生物合成，抑制氧化酶和过氧化酶的活性，引起细胞内过氧化氢积聚导致细胞亚微结构的变性和细胞坏死。对白色念珠菌则可抑制其自芽胞转变为具侵袭性的菌丝形式的过程。