
簡(jiǎn)要描述:Bifonazole 60628-96-8Bifonazole acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase).
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| 品牌 | absin | CAS | 60628-96-8 |
|---|---|---|---|
| 分子式 | C22H18N2 | 純度 | 99% |
| 分子量 | 310.39 | 貨號(hào) | abs47027542 |
| 規(guī)格 | 25mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | acts to destabilize the fungal cytochrom | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Bifonazole 60628-96-8
| 產(chǎn)品描述 | |
| 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. |
| 純度 | 99% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | lian苯芐唑;Bay H-4502 |
| 外觀 | 白色或類白色粉末 |
| 可溶性/溶解性 | DMSO : 58 mg/mL (186.9 mM) Ethanol : 16 mg/mL (51.5 mM) |
| 生物活性 | |
| 靶點(diǎn) | CYP51 |
| In vitro(體外研究) | 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). 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. 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. 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. |
| In vivo(體內(nèi)研究) | 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. |
| 參考文獻(xiàn) | |
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| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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