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Bifonazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:60628-96-8
包装与价格:
包装价格(元)
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
联苯苄唑
Bay H-4502
产品介绍
Bifonazole 是咪唑类抗真菌剂。

产品描述

Bifonazole acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. This is vital in the cell membrane structure of the fungus. Its inhibition leads to cell lysis. The disruption in production of ergosterol disrupts the cell membrane and causes holes to appear. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out.

体外活性

Bifonazole, a broad spectrum antifungal agent, inhibits monooxygenase activity and induces a type II binding spectrum in 2B4dH(H226Y), a modified enzyme previously crystallized in the presence of 4-(4-chlorophenyl)imidazole (CPI). [1] Bifonazole (40 mM) releases Ca2+ from the store sensitive to 1 mM thapsigargin, an endopolasmic reticulum Ca2+ pump inhibitor. Bifonazole (40 mM) per se induces capacitative Ca2+ entry while reduces 1 mM thapsigargin-induced capacitative Ca2+ entry. [2] Bifonazole is calmodulin antagonists which most effectively reduce glycolysis and ATP level in B16 melanoma cells. Bifonazole acts through allosteric regulation and detachment of glycolytic enzymes from cytoskeleton. [3] Bifonazole blocks PGE2 formation induced by 2 ?μm and 4?μm arachidonic acid clearly better than at 6 or 10?μm of the agonist. Bifonazole shows the same characteristics in MC3T3-E1 and UMR-106 cells stimulated by ionomycin or various concentrations of arachidonic acid. [4]

体内活性

Bifonazole, but not clotrimazole, exhibits the characteristics of a peroxisome proliferator including hepatomegaly (increase in liver:body weight ratio), up to a 4-fold induction of lauric acid omega-hydroxylase activity and an 8-fold induction of palmitoyl-CoA oxidation by rat liver peroxisomes. Bifonazole also induces P402B1/2B2, P4503A and P4501A1, but not P4502E1. [5]

Cas No.

60628-96-8

分子式

C22H18N2

分子量

310.39

别名

联苯苄唑;Bay H-4502

储存和溶解度

DMSO:58 mg/mL (186.9 mM)
H2O:<1 mgml
Ethanol:16 mg/mL (51.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years