High Throughput P450 Inhibition Kits
These human Cytochrome P450 High Throughput Inhibitor Screening Kits
are designed to rapidly screen for potential inhibitors of Cytochrome
P450 catalytic activity. Each kit provides all the necessary components
and instructions for measuring the IC50 value of up to 38 test compounds
in 96-well plates. The inhibitor screening kit includes the following
components: recombinant human P450, (Supersomes™ Enzymes) fluorescent
P450 substrate, positive control inhibitor, metabolite standard, NADPH
regenerating system, reaction buffer, stop reagent, control membrane protein,
and an instruction manual.
Follow this link
to learn more about high throughput screening methodology for human cytochrome
P450 inhibition. This link
will provide a detailed method for those who want to use the individual
components supplied by BD Biosciences to run their High Throughput Assays.
This
bulletin describes the methodology for CYP1A2, CYP2A6, CYP2B6, CYP2C8,
CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 assays.
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HTS P450 Inhibition Kit
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Catalog No.
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Enzyme (pmol/well)
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Substrate (µM)
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NADP+ (µM)
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Glucose-6-Phosphate (mM)
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Magnesium Chloride
Hexahydrate (mM)
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Glucose-6-Phosphate Dehydrogenase (Units/mL)
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3A4/BFC
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459100
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1
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50
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8.1
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0.4
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0.4
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0.2
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3A4/BQ
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459110
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1.5
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40
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8.1
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0.4
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0.4
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0.2
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3A4/DBF
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459120
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0.2
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1
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8.1
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0.4
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0.4
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0.2
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2D6/AMMC
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459200
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1.5
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1.5
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8.1
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0.4
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0.4
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0.2
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2C8/DBF
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459320
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1.8
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1
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8.1
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0.4
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0.4
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0.2
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2C9/MFC
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459300
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1
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75
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8.1
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0.4
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0.4
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0.2
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2C19/CEC
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459400
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1
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25
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8.1
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0.4
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0.4
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0.2
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2A6/Coumarin
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459420
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1
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3
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8.1
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0.4
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0.4
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0.2
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1A2/CEC
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459500
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1
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5
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8.1
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0.4
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0.4
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0.2
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2B6/EFC
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459220
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1
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2.5
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8.1
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0.4
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0.4
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0.2
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2E1/MFC
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459620
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1
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70
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8.1
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0.4
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0.4
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0.2
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96 Well Assay Plates
For all fluorescent P450 assays we recommend the BD Falcon 96 well black
plates (Cat. No. 353241(25/pk, 100/cs)) and lids (Cat. No. 353958). These
plates are not a component of the Gentest P450 Inhibition kits and must
be purchased separately.
Please note these products are available through your Fisher or VWR
representative.
The equivalent catalog number for these vendors are:
Fisher 96 well black plates (Cat. No. 02-683-140) and lids (Cat. No. 08-772-113).
VWR 96 well black plates (Cat. No. 22221-572) and lids (Cat. No. 62406-486).
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