Cyprotex's Cytochrome P450 Time Dependent Inhibition IC50 Shift assay is able to identify both reversible and time-dependent inhibitors and discriminate between compounds which cause reversible and irreversible inhibition or both.
IC50 shiftIn this chapter we have provided a step-by-step protocol for a time-dependent inhibition (TDI) IC 50 shift assay using stable isotopic labeled probe substrates. The assay is performed in a 96-well format and can be fully automated and extended to a 384-well format if desired. ...
Time dependent CYP inhibition (IC50shift) Time dependent CYP inhibition (kinact/KI) Data Data from Cyprotex's Cytochrome P450 Inhibition Assay Known CYP inhibitors were screened in Cyprotex's Cytochrome P450 Inhibition assay in 3 separate assays. ...
CYP Time-dependent inhibition (TDI)using an IC50 shift assay with stable isotopic labeled substrate probes to facilitate liquid chromatography/mass spectrometry... GW Caldwell,Z Yan 被引量: 1发表: 2014年 Use of stable isotope labeled probes to facilitate liquid chromatography/mass spectrometry based ...
Time dependent CYP inhibition (IC50shift) Time dependent CYP inhibition (kinact/KI) Data Data from Cyprotex's Cytochrome P450 Inhibition Assay Known CYP inhibitors were screened in Cyprotex's Cytochrome P450 Inhibition assay in 3 separate assays. ...
Assessing Cytochrome P450 Time-Dependent Inhibition (IC50 Shift Assay) Using Both Diluted and Non-Diluted MethodsEvaluation of the time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes is very important for understanding the drug鈥揹rug interactions. TDI is usually studied by measuring the...
IC50 shiftIn this chapter we have provided a step-by-step protocol for a time-dependent inhibition (TDI) IC50 shift assay using stable isotopic labeled probe substrates. The assay is performed in a 96-well formdoi:10.1007/978-1-62703-742-6-19Gary W. Caldwell...
HUMAN HEPATOCYTE BASED CYP3A4 INHIBITION IC50-SHIFT ASSAY PREDICTION OF CLINICAL DRUG-DRUG INTERACTIONSJacob A. Olsen
Stresser, Validation of cytochrome P450 time- dependent inhibition assays: a two-time point IC50 shift approach facilitates k inact assay design, Xenobiotica 39 (2009) 99-112.Perloff, E. S., Mason, A. K., Dehal, S. S., Blanchard, A. P., Morgan, L., Ho, T., Dandeneau, A., ...
The enzyme inactivation kinetics of mechanism-based inhibitors of CYP2C8 were assessed using multiple pre-incubation times (0, 5, 10, 15, 20, and 30 min) and multiple inhibitor concentrations with human liver microsomes (1 mg/ml) followed by an enzyme activity assay using amodiaquine (at a...