产品说明书

FCCP

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Chemical Structure| 370-86-5 同义名 : Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone;Trifluoromethoxy carbonylcyanide phenylhydrazone;para-Trifluoromethoxyphenylhydrazone, Carbonyl Cyanide.;p-Trifluoromethoxyphenylhydrazone, Carbonyl Cyanide;Carbonyl Cyanide para Trifluoromethoxyphenylhydrazone;Carbonyl cyanide-p-trifluoromethoxyphenylhydrazone
CAS号 : 370-86-5
货号 : A194814
分子式 : C10H5F3N4O
纯度 : 99%+
分子量 : 254.168
MDL号 : MFCD00009699
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(413.11 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 30 mg/mL(118.03 mM),注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:

IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

生物活性
描述 FCCP is a potent mitochondrial oxidative phosphorylation uncoupler which exhibits uncoupling effects at concentrations down to 10 -8 molar in mouse liver mitochondria[1]. Treatment with 5μM FCCP led to a reduction of ATP levels and ROS production and stimulated mitochondrial biogenesis related genes including Pgc-1α, mitochondrial genes such as Tfam and COXIV in hepatic stellate cells[2]. FCCP at concentration of 62.5nM and 125nM significantly reduced the mitochondrial membrane potential in the cytoplasmic and cortical region, as well as decreased ATP level of 8-cell embryos[3]. The processing of mutant APP in K695sw cells and wild-type APP in K695 cells was inhibited post treatment with 5μM FCCP for 4h[4].
作用机制 FCCP is a protonophore which can induce ionic currents carried by Na+ and H+ and depolarization dependent on the plasmalemmal proton gradient.[5]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Hep3B cells 10 μM Function assay Stimulation of state 4 cellular respiration in human Hep3B cells at 10 uM in presence of oligomycin 22938093
MDA-MB-231 cells 1 uM Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation/viability at 1 uM 23245650
SH-SY5Y cells 10 μM Function assay 10 mins Induction of mitochondrial membrane potential loss in human SH-SY5Y cells at 10 uM incubated for 10 mins in presence of 0.2 uM CsA by TMRE dye based assay 25265024
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00613860 Emphysema COP... 展开 >>D 收起 << Phase 3 Unknown December 2011 Germany ... 展开 >> Charite, University of Berlin Recruiting Berlin, Germany, 10117 Contact: Christian Witt, MD, PhD    +49 (030) 450 565 022    pneumologie@charite.de    Contact: Bernd Schmitt, MD    +49 (030) 450 565 02    pneumologie@charite.de    Thoraxklinik, University of Heidelberg Recruiting Heidelberg, Germany, 69190 Principal Investigator: Felix JF Herth, MD, PhD          Medical Center Nürnberg Recruiting Nürnberg, Germany, 90340 Contact: Joachim Ficker, MD, PHD    +49 (911) 398-2675    ficker@klinikum-nuernberg.de    Contact: Manfred Wagner, MD    +49 (911) 398-0    Manfred.Wagner@klinikum-nuernberg.de 收起 <<
NCT00176540 Fatigue Unspe... 展开 >>cified Adult Solid Tumor, Protocol Specific Unspecified Childhood Solid Tumor, Protocol Specific 收起 << Not Applicable Terminated(slow accrual) - United States, New Jersey ... 展开 >> Cancer Institute of New Jersey at Hamilton Hamilton, New Jersey, United States, 08690 Cancer Institute of New Jersey at UMDNJ - Robert Wood Johnson Medical School New Brunswick, New Jersey, United States, 08903 收起 <<
NCT01187147 Asthma Not Applicable Completed - Hong Kong ... 展开 >> University of Hong Kong Queen Mary Hospital Hong Kong, Hong Kong, 0 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.93mL

0.79mL

0.39mL

19.67mL

3.93mL

1.97mL

39.34mL

7.87mL

3.93mL

参考文献

[1]HEYTLER PG, PRICHARD WW, et al. A new class of uncoupling agents--carbonyl cyanide phenylhydrazones. Biochem Biophys Res Commun. 1962 May 4;7:272-5.

[2]Guimarães EL, Best J, et al. Mitochondrial uncouplers inhibit hepatic stellate cell activation. BMC Gastroenterol. 2012 Jun 11;12:68.

[3]Zander-Fox DL, Fullston T, et al. Reduction of Mitochondrial Function by FCCP During Mouse Cleavage Stage Embryo Culture Reduces Birth Weight and Impairs the Metabolic Health of Offspring. Biol Reprod. 2015 May;92(5):124.

[4]Connop BP, Thies RL, et al. Novel effects of FCCP [carbonyl cyanide p-(trifluoromethoxy)phenylhydrazone] on amyloid precursor protein processing. J Neurochem. 1999 Apr;72(4):1457-65.

[5]Park KS, Jo I, et al. FCCP depolarizes plasma membrane potential by activating proton and Na+ currents in bovine aortic endothelial cells. Pflugers Arch. 2002 Jan;443(3):344-52. Epub 2001 Oct 6.