联苯苄唑, HMG-CoA 还原酶抑制剂

真菌抑制剂

1篇引用文献

COA

级别和纯度:

10mM in DMSO

CAS编号: 60628-96-8
分子式: C₂₂H₁₈N₂
分子量: 310.39

有货

库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
B407805-1ml	1ml	现货

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Compound libraries (12333)

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基本描述

英文别名	Bay h 4502 \| 1-([1,1'-biphenyl]-4-ylphenylmethyl)-1H-imidazole
规格或纯度	10mM in DMSO
英文名称	Bifonazole
生化机理	联苯苄唑（Bay h 4502）是一种取代咪唑类抗真菌剂。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	抑制剂
作用机制	HMG-CoA 还原酶抑制剂
产品介绍	Bifonazole 是一种抗真菌剂和前列腺芳香化酶抑制剂，IC50为1.6 μM。An imidazole antifungal agent and calmodulin antagonist. Information Bifonazole Bifonazole (Bay h 4502) is a substituted imidazole antifungal agent. In vitro 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 \u2009μm and 4\u2009μm arachidonic acid clearly better than at 6 or 10\u2009μm 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 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. Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥99%

产品属性

ALogP	4.8

关联靶点（人）

CYP3A4 Tclin 细胞色素P450 3A4(Cytochrome P450 3A4) (1 活性数据)

点击查看靶蛋白信息： CYP3A4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

CYP51A1 Tchem 羊毛甾醇14-α脱甲基酶(Lanosterol 14-alpha demethylase) (1 活性数据)

点击查看靶蛋白信息： CYP51A1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

CYP17A1 Tclin 类固醇 17-α-羟化酶/17,20 裂解酶(Steroid 17-alpha-hydroxylase/17,20 lyase) (2 活性数据)

点击查看靶蛋白信息： CYP17A1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

分子类型	小分子
Isomeric SMILES	C1=CC=C(C=C1)C2=CC=C(C=C2)C(C3=CC=CC=C3)N4C=CN=C4
分子量	310.39
Reaxy-Rn	618427
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=618427&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 129 mg/mL warmed with 50ºC Water: bath (199.79 mM); Water: Insoluble; Ethanol: Insoluble;
熔点	149 °C

安全和危险性（GHS）

象形图	GHS07
信号词	Warning
危险声明	H302: 吞食有害
预防措施声明	P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P317: 如果被吞咽：请寻求医疗帮助。
WGK Germany	3
RTECS	NI3517000
Merck Index	1213

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

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引用文献

1. Susu Lin, Bingbing Ma, Qilin Gao, Jian Yang, Gang Lai, Runhao Lin, Bingxian Yang, Bing-Nan Han, Lian-Hua Xu. (2022) The 16α-Hydroxylation of Progesterone by Cytochrome P450 107X1 from Streptomyces avermitilis. CHEMISTRY & BIODIVERSITY, 19 (5): (e202200177). [PMID:35426465] [10.1002/cbdv.202200177]