Escape the limits of fluorescence and Go luminescent - Assay your entire compound library without compromise and get high predictive value and high throughput, all without concern about fluorescent interference.
P450-Glo™ Assay Systems are designed to bring the power and clarity of luminescence to measure the effects of all your compounds on cytochrome P450 enzyme activity.
Review our numbers and compare with your own, then request an evaluation of P450-Glo Assay System and prove to yourself that it is the best way to deliver clear results brightly every time.
Complete P450-Glo Screening Systems are now available for 1A2, 2C9, 2C19, 2D6 and 3A4. Learn more...
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Why Choose Luminescence over Fluorescence?
Luminescent assays are exquisitely sensitive and not limited by overlap between the fluorescent properties of analytes and assay components. Typically 5% or more of a chemical library’s compounds have fluorescent properties that confound analysis with fluorescent probes. By using luminescence entire libraries can be screened without the intrinsic limitations of fluorescent assay methodologies.
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CYP3A4 CYP2C9 CYP2C19 CYP1A2 CYP2D6 CYP1A1 |
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Clear Results from Luminescent Output.
P450-Glo™ produces clear signals when the assay is applied to specific
cytochrome CYP450.
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Luciferin-BE Luciferin-H Luciferin-H EGE Luciferin-ME Luciferin-ME EGE Luciferin-CEE Luciferin-PFBE Luciferin-PPXE |
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Get high signal to background ratios and high predictive value.
Typical cytochrome P450 assay protocols recommend >0.5pmole of enzyme per well. Under these conditions, Z′-factor values of greater than 0.8 are routinely obtained using P450-Glo™ CYP450 Assay Systems. 0.25 &pico;moles of recombinant CYP 2C9 was assigned using the P450-Glo CYP 2C9 Assay.
IC50 Values Compared with Conventional Assays
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| CYP450/substrate Combination |
IC50 Values |
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| αNA | KET | SUL | ERT | VRP | |
| CYP1A1/Luciferin-CEE | 0.4 | 0.1 | 0.1 | ||
| CYP1A1/phenacetin(2) | 0.2 | ||||
| CYP1A2/Luciferin-ME | 0.1 | ||||
| CYP1A2/imaprine(1) | 0.05 | ||||
| CYP2C8/Luciferin-ME | 1.4 | ||||
| CYP2C8/phenanthrene(1) | 8.9 | ||||
| CYP2C9/Luciferin-H | 0.1 | ||||
| CYP2C9/diazepem(1) | 0.5 | ||||
| CYP2C9/phenanthrene(1) | 0.7 | ||||
| CYP3A4/Luciferin-BE | 0.06 | 1.2 | 0.1 | ||
| CYP3A4/diazepem(1) | 0.5 | ||||
| CYP3A4/phenanthrene(1) | 0.03 | ||||
| CYP3A4/testosterone(1) | 0.04 | ||||
| CYP3A4/BFC(3) | 0.005 | 4.6 | 0.4 | ||
| CYP3A4/DBF(3) | 0.002 | 26.5 | 4.2 | ||
| CYP3A4/testosterone | 0.04(1) | ~30(3) | 24(4) | ||
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Chart Legend: αNA: α-naphthoflavone KET: Ketoconazole SUL: Sulfaphenazole ERT: Erythromycin VRP: Verapamil References: (1) Sai Y, Dai R, Yang TJ, Krausz KW, Gonzalez FJ, Gelboin HV, Shou M. Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica. 2000 Apr;30(4):327-43. (2) Tassaneeyakul W, Birkett DJ, Veronese ME, McManus ME, Tukey RH, Quattrochi LC, Gelboin HV, Miners JO. Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. J. Pharmacol. Exp. Ther. 1993 Apr;265(1):401-7. (3) Stresser DM, Blanchard AP, Turner SD, Erve JC, Dandeneau AA, Miller VP, Crespi CL. Substrate-dependent modulation of CYP3A4 catalytic activity: analysis of 27 test compounds with four fluorometric substrates. (2000) Drug Metab. Dispos. 28 (12):1440-48 (4) Wang E, Lew K, Barecki M, Casciano CN, Clement RP, Johnson WW. Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. (2001) Chem. Res. Toxicol. 14 (12):1596-1603 |
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