Factsheet transil_xl_agp v8.ai

FactSheet TRANSIL_XL_AGP V8.ai 1 29.08.2012 14:31:25 TRANSILXL
AGP Binding Kit
FEATURES AND BENEFITS
 Fast, requires only 20 minutes total assay time  Accurate, measures the affinity of drug candidates to  -acid glycoprotein (AGP) to predict plasma protein binding under diverse  Reliable with highly reproducible results, and robust correlation to equilibrium dialysis method. Fully quality-controlled binding  Rapid compound quantification due to immoblized plasma proteins  Kit includes a spreadsheet for calculation of final results and traffic TECHNICAL DESCRIPTION
The TRANSILXL AGP Binding Kit estimates the binding of drugs to  -acid glycoprotein (AGP) and is essential for predicting plasma protein binding under disease states. The assay kit measures the affinity constant (K ) of drugs to AGP and hence allows the calculation of AGP under disease dependent protein concentration ranging from 0.4 to 2.8 g/L. In combination with TRANSILXL HSA Binding Kit it is possible to obtain accurate prediction of plasma protein binding in a highly controlled and reproducible assay environment.
The kit consists of ready-to-use 96-well microtiter plates. One plate can be used for measuring AGP binding of up to 12 compounds. The assay requires only 5 steps: (i) addition of drug candidate, (ii) mixing and incubation for 12 minutes, (iii) removal of beads by centrifugation, (iv) sampling of supernatant, and (v) quantification of CAPABILITIES
  Affinity constant (K ) of drugs to AGP   Unbound fraction of drug in AGP solution   Unbound fraction of drug in plasma   Concentration dependet plasma protein binding Sovicell
Deutscher Platz 5b 04103 Leipzig t. +49 341 520 44 0 f. +49 341 520 44 12 e. [email protected] www.sovicell.com
FactSheet TRANSIL_XL_AGP V8.ai 2 29.08.2012 14:31:28 Validation of the TRANSILXL AGP Binding Kit
Human serum albumin (HSA) and human 1-acid glycoprotein are the most important plasma binding proteins. TRANSIL binding assays are available for both proteins. The TRANSILXL AGP Binding Kit employs immobilized AGP with a random orientation. This makes sure that all binding sites are available and that the assay reproduces exactly the binding of drugs to AGP in solution (fig. 2). The TRANSILXL AGP Binding assay is designd to predict plasma protein binding in conjunction with the TRANSILXL HSA Binding assay (fig. 3) and to model plasma protein binding under a broad range of disease conditions. Differences in relation to plasma binding arise through variations in plasma composition, due to lipids blocking binding sites in native plasma, and occasionally due to binding to other plasma proteins with low abundance. Figure 4 illlustrates that AGP can contribute primarily to plasma binding of acidic or neutral drugs.
2: Comparison of AGP binding measured using the Fig. 3: Comparison of plasma protein binding predictions TRANSILXL AGP Kit and by dialysis with AGP.
based on the TRANSILXL HSA and AGP assay and serum HSA and AGP contribution to plasma protein binding represented as decrease in drug unbound as a consequence of binding to AGP. AMI: amitriptyline, CHL: chlorpromazin, DIC: diclofenac, DIG: digitoxin, DIS: disiopyramid, FLX: fluoxetine, FLP: flurbiprofen, FUR: furosemid, IMI: imipramin, IND: indomethacin, KET: ketoprofen Wdh, NAX: naxopren, PAC: paclitaxel, PHE: phenylbutazon, PRG: progesteron, PRP: propranolol, SUL: sulfasalazine, VER: verapamil, VIN: vincristine, WAR: warfarin PRODUCT INFORMATION
Order Number
Sovicell
Deutscher Platz 5b 04103 Leipzig t. +49 341 520 44 0 f. +49 341 520 44 12 e. [email protected] www.sovicell.com

Source: http://www.sovicell.at/factsheets/FactSheet%20TRANSIL_XL_AGP%20V8.pdf