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伏立康唑, 细胞色素 P450 51 抑制剂

P450 Selective Inhibitors | Chemicals
  • CAS编号: 137234-62-9
  • 分子式: C16H14F3N5O
  • 分子量: 349.31
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货号 (SKU) 包装规格 是否现货 价格 数量
V409051-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Voriconazole (UK-109496)
生化机理 伏立康唑(UK-109496)是一种新型三唑衍生物,与氟康唑和伊曲康唑相似,通过抑制真菌细胞色素 P-450 依赖性 14-α-甾醇脱甲基酶介导的麦角甾醇合成发挥作用。
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 细胞色素 P450 51 抑制剂
产品介绍

Voriconazole (伏立康唑; UK-109496) 是第二代三唑类抗真菌化合物,可作用于严重的真菌感染。An antifungal CYP2C9 inhibitor

Information

Voriconazole (UK-109496) is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungalcytochrome P-450-dependent,14-alpha-sterol demethylase-mediated synthesis of ergosterol.
In vitro

Voriconazole is active against certain opportunistic filamentous and dimorphic fungi (molds) and yeasts. Voriconazole in vitro activities are higher than or similar to those of itraconazole and amphotericin B for most of the molds tested, with the exceptions of R. arrhizus and S. schenckii. Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates.

In vivo

Voriconazole is significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised guinea pig with pulmonary aspergillosis. Voriconazole also has been shown to be effective in guinea pigs with experimental pulmonary or intracranial infections caused by C. neoformans. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) significantly reduces the colony counts in the tissues of selected Guinea pigs compared with those in the tissues of the controls. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) also results in reductions in colony counts in tissues compared with those in the tissues of Guinea pigs treated with caspofungin acetate (the difference is not statistically significant) and improves the survival times but does not sterilize tissues. Voriconazole (5 mg/kg/day, i.p.) combined with caspofungin acetate (CAS) at either dose reduces colony counts in tissues 1,000-fold over those for the controls and are the only regimens that significantly reduces the numbers of positive cultures.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 1.5

关联靶点(人)

CYP2B6 Tchem 细胞色素 P450 2B6(Cytochrome P450 2B6) (3 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP46A1 Tchem 胆固醇24-羟化酶(Cholesterol 24-hydroxylase) (8 活性数据)
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 C[C@@H](C1=NC=NC=C1F)[C@](CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O
PubChem CID 71616
分子量 349.31
Reaxy-Rn 7694998

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 87 mg/mL (307.04 mM); Ethanol: 3 mg/mL (10.58 mM); Water: Insoluble;
比旋光度 -58.0 to -62.0 deg(C=1, MeOH)
沸点 ~508.6° C at 760 mmHg
熔点 128-134°C

安全和危险性(GHS)

象形图 GHS06,   GHS08,   GHS09
信号词 Danger
危险声明

H301: 吞咽会中毒

H351: 怀疑引起遗传缺陷

H373: 通过长时间或反复暴露对器官造成损害

H412: 对水生生物有害并具有长期持续影响

H400: 对水生生物有剧毒

H360: 可能损害生育力或未出生的孩子

H361: 怀疑破坏生育力或未出生的孩子

预防措施声明

P273: 避免释放到环境中。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P321: 特殊处理(请参阅此标签上的...)。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P391: 收集溢出物

P330: 漱口

P203: 使用前,获取、阅读并遵守所有安全说明。

P301+P316: 如果吞咽:立即寻求紧急医疗救助。

P318: 如果暴露或担心,请就医。

P319: 如果你感到不适,请寻求医疗帮助。

WGK Germany 3
RTECS UV9145000
Merck Index 10033

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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