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Substrate activity at rat NADPH-cytochrome P450 oxidoreductase expressed in supersomes assessed as compound cleavage after 90 mins in anaerobic condition by HPLC analysis
Assay data:15 Tested
SummaryPubMed CitationRelated BioAssays by Target
Substrate activity at rat NADPH-cytochrome P450 oxidoreductase expressed in supersomes assessed as compound cleavage after 24 hrs in anaerobic condition by HPLC analysis
Assay data:1 Tested
Prodrug conversion in pH 7.4 PBS buffer assessed as NADPH-cytochrome P450 reductase (unknown origin) mediated FdUrd release by measuring Km at 0.62 mM in the presence of beta-NADPH measured after 2 hrs under aerobic condition by Lineweaver-Burk plot analysis
Prodrug conversion in pH 7.4 PBS buffer assessed as NADPH-cytochrome P450 reductase (unknown origin) mediated FdUrd release by measuring Km at 0.62 mM in the presence of beta-NADPH measured after 2 hrs under hypoxic condition by Lineweaver-Burk plot analysis
Prodrug conversion in pH 7.4 PBS buffer assessed as NADPH-cytochrome P450 reductase (unknown origin) mediated FdUrd release by measuring Vmax at 0.62 mM in the presence of beta-NADPH measured after 2 hrs under aerobic condition by Lineweaver-Burk plot analysis
Prodrug conversion in pH 7.4 PBS buffer assessed as NADPH-cytochrome P450 reductase (unknown origin) mediated FdUrd release by measuring Vmax at 0.62 mM in the presence of beta-NADPH measured after 2 hrs under hypoxic condition by Lineweaver-Burk plot analysis
Prodrug conversion assessed as NADPH-cytochrome P450 reductase (unknown origin) mediated F-OH formation by measuring Vmax at 0.93 mM in the presence of beta-NADPH measured after 15 mins under hypoxic condition by Lineweaver-Burk plot analysis
Prodrug activation in pH 7.4 PBS buffer assessed as 3.3 ug/mL NADPH-cytochrome P450 reductase (unknown origin) mediated FdUrd formation at 0.62 mM in the presence of beta-NADPH measured after 2 hrs under aerobic condition by reverse phase HPLC
Prodrug activation in pH 7.4 PBS buffer assessed as 3.3 ug/mL NADPH-cytochrome P450 reductase (unknown origin) mediated FdUrd formation at 0.62 mM in the presence of beta-NADPH measured after 2 hrs under hypoxic condition by reverse phase HPLC relative to control
Assay data:2 Tested
Substrate activity at human CPR expressed in baculovirus expression system assessed as reduction rate by measuring umol of NADPH utilized per umol of enzyme at 10 uM preincubated for 3 mins followed by NADPH addition measured at 2 secs interval for 5 mins by UV-Vis spectroscopy
Assay data:8 Tested
Prodrug activation in mouse liver microsomes assessed as CYP450 reductase-mediated SN-38 release at 5 uM after 6 hrs in presence of NADPH by HPLC method
Induction of recombinant human CPR-mediated superoxide generation assessed as one-electron reduction of compound by measuring SOD-inhibitable reduction of succinoylated cytochrome c per 2 mU enzyme at 100 umol/ml by spectrophotometric analysis (Rvb = 0.2 +/- 0.1 micromol/L/min)
Assay data:7 Tested
Drug metabolism in pH 7.4 PBS assessed as rat P450 oxidoreductase-mediated compound hydrolysis preincubated for 20 mins followed by protocatechuate 3,4-dioxygenase addition to create anoxic condition and subsequent addition of P450 oxidoreductase in presence of NADPH after 24 hrs by HPLC method
Assay data:3 Tested
Prodrug activation assessed as supersomal P450 oxido-reductase (unknown origin)-mediated CA4 level at 2.5 uM in presence of 0.5% O2 condition after 2 mins by HPLC method
Substrate activity at recombinant human CPR expressed in baculovirus infected insect cells assessed as compound reduction rate by measuring NADPH consumption per umol of enzyme preincubated for 3 mins followed by NADPH addition measured for 5 mins at 2 sec time interval by UV-Visible spectroscopic method
Assay data:23 Tested
Substrate activity at CPR in human L02 cells assessed as CPR-mediated one-electron reduction of compound by measuring cell growth inhibition treated for 24 hrs measured after 72 hrs by MTT assay
Assay data:2 Active, 11 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Substrate activity at CPR in human L02 cells assessed as CPR-mediated one-electron reduction of compound by measuring cell growth inhibition at 20 to 100 uM treated for >8 hrs measured after 72 hrs by MTT assay
Assay data:1 Active, 1 Tested
Substrate activity at CPR in human L02 cells assessed as CPR-mediated one-electron reduction of compound by measuring ROS production after 1 to 3 hrs by DCFH-DA staining based flow cytometry
Substrate activity at CPR in human L02 cells assessed as CPR-mediated one-electron reduction of compound by measuring ROS production at 10 uM after 1 to 3 hrs by DCFH-DA staining based flow cytometry
Metabolic stability in rat liver S9 fraction assessed as NADPH CYP450 reductase-mediated compound metabolism by measuring compound remaining in presence of NADPH at 20 uM after 30 mins by HPLC method
Assay data:11 Tested
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