福司氟康唑 - CAS:194798-83-9 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	福司氟康唑
英文名称:	Fosfluconazole
别名:	福司氟康唑 [2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-yl] dihydrogen phosphate
CAS No:	194798-83-9	分子式:	C₁₃H₁₃F₂N₆O₄P	分子量:	386.25
CAS No:	194798-83-9
分子式:	C₁₃H₁₃F₂N₆O₄P
分子量:	386.25

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F10203 福司氟康唑 ≥98% (psaitong)

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包装规格：

10mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO（6.2 mg/mL 超声，加热)

产品描述：

基本信息

产品编号：F10203
产品名称：Fosfluconazole
CAS:	194798-83-9	储存条件	粉末	-20℃	四年

分子式：	C13H13F2N6O4P		溶于液体	-80℃	两年
分子量	386.25			-20℃	一个月
化学名：	1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-((1H-1,2,4-triazol-1-yl)methyl)ethyl dihydrogen phosphate
Solubility (25°C)	体外	DMSO	19mg/mL (49.19mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内	现配现用
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.5890mL	12.9450mL	25.8900mL
5mM	0.5178mL	2.5890mL	5.1780mL
10mM	0.2589mL	1.2945mL	2.5890mL

生物活性

产品描述	Fluconazole 的前药，广泛用作抗真菌剂。
靶点/IC₅₀	Antifungal
体外研究	To investigate the polarized bioconversion and the Transwell transport of phosphate prodrugs in Caco-2 monolayer, 10μM Fosfluconazole or Fosphenytoin is dosed either in the apical or basal compartment in Transwell plates. Both prodrugs are efficiently cleaved in the apical compartment after a 2h incubation. To further investigate the kinetics of ALP-mediated bioconversion, the concentration-dependent ALP-mediated bioconversions are conducted to determine the MichaelisMenten constant (Km) of prodrug bioconversion in Caco-2 monolayers. The saturation curves of Fosphenytoin and Fosfluconazole with the concentration increase are found. The estimated Km values of Fosphenytoin and Fosfluconazole are 1160 and 357μM, respectively.
体内研究	The apparent half-life for Fosfluconazole bioconversion in intestinal mucosa scraps is 10 min. Fluconazole (FLCZ) is an antifungal agent that is efficacious in the treatment of fungal peritonitis. Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study are to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ is administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ is detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration is lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations are analyzed using a two-compartment model in which the distribution volume of the peripheral compartment is fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients.

推荐实验方法(仅供参考)

激酶实验：

Kinase Assay

An aliquot of 200μL of mucosa scrap lysate solution is mixed with 100mM phosphate buffer, pH 7.4, to a final volume at 1ml. The concentration of the test compounds (Fosphenytoin and Fosfluconazole) is 10μM. The incubation medium is prewarmed at 37°C before the reaction is initiated by addition of the tested compounds. An aliquot of 100μL is collected from the incubation vial at the time points 0, 5, 10, 20, 30, 45, and 60 min and transferred to a 96-well plate, in which 100μL of Acetonitrile is prefilled to terminate the reaction. The samples are diluted 5-fold with acetonitrile containing 1μM Tolbutamide as an analytical internal standard. The samples are centrifuged at 4000 rpm for 5 min to precipitate protein.The supernatant is transferred to a new 96-well plate for concentration analysis by liquid chromatography/tandem massspectrometry (LC/MS/MS).

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果