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TRANSIL Plasma Protein Binding Assays

The Kit estimates the binding of drugs to human serum albumin (HSA) and predicts the plasma protein binding. The assay kit measures the dissociation constant (KD) of drugs to albumin and hence allows the calculation of albumin binding even under disease and physiological states that alter the albumin content of human serum. In combination with our TRANSIL AGP Binding Kit it is possible to obtain accurate prediction of plasma protein binding in a highly controlled and reproducible assay environment. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0210-2096

The Kit estimates the binding of drugs to rat serum albumin (RSA) and predicts the plasma protein binding. The assay kit measures the KD of drugs to albumin and hence allows the calculation of albumin binding even under disease and physiological states that alter the albumin content of human serum. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0210-2096

The Kit estimates the binding of drugs to human α1 acid glycoprotein (AGP/AAG). The assay kit measures the affinity constant (KD) of drugs to AGP and hence allows the calculation of AGP binding even under disease and physiological states that substantially alter the AGP content of human serum. In combination with our TRANSIL HSA Binding Kit it is possible to obtain accurate prediction of plasma protein binding in a highly controlled and reproducible assay environment. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0211-2096

Transil MSA Binding Kit

The Kit estimates the binding of drugs to mouse serum albumin (MSA) and predicts the plasma protein binding. The assay kit measures the affinity constant (KD) of drugs to albumin and hence allows the calculation of albumin binding even under disease and physiological states that alter the albumin content of human serum. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0230-2096

The Kit estimates the binding of drugs to human serum albumin (HSA) and human alpha-1 glycoprotein (AGP/AAG) at a physiological ratio to predict plasma protein binding. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0212-2096

Transil High Sensitivity Binding Kits

Compounds binding strongly to plasma proteins frequently result in overly small compound concentrations that are difficult to measure accurately. Also, time to equilibrium increases the stronger compounds bind to plasma. The TRANSIL High sensitivity binding kit solves this by introducing another binding matrix and analysing the binding equilibrium between this solid-phase matrix (natural membranes) and the liquid phase including plasma.

Highly lipophilic and sticky compounds also create notorious difficulties in plasma protein binding assays. The TRANSIL High sensitivity binding kit addresses this by providing plasma in all assay compartments.

Thus, the TRANSIL High Sensitivity Binding Kit accurately determines the unbound fraction of drugs that are tightly bound to plasma proteins - even when the unbound fraction is well below 1%. Also, the TRANSIL assay yields high recovery for drugs that exhibit too high unspecific binding in other assay systems, or precipitate because of low solubility. The kit determines the fraction of drug bound to plasma indirectly by measuring the partitioning of drug between the plasma proteins and artificial cell membranes.     TMB-0400-0135     TMB-0400-0335     TMB-0400-2535     TMB-0410-0135     TMB-0410-0335     TMB-0410-2535  

TRANSIL Membrane Binding & Permeability Assays

The kit estimates the binding of drugs to brain tissue and predicts the disposition of drugs into brain. It measures the affinity of drugs to reconstituted porcine brain membranes. The brain membrane affinity is used to estimate the brain tissue binding and to predict the brain-to-plasma distribution via a hybrid model that also incorporates the drug’s polar surface area and its plasma protein binding. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0110-2096     TMP-0110-2196

The kit measures the affinity of drugs to phosphatidylcholine membranes. It is not only a screening tool to predict intestinal permeability coefficients, but also to predict compounds’ tissue binding. As drug-membrane interactions are key to both the process of membrane permeability and to binding to and permeating into the cell membranes of tissues the assay kit is an ideal tool to predict intestinal permeability rates as well as the volume of distribution early in drug discovery phase. Internal quality controls provide easy assessment of recovery, experiment and data quality.     TMP-0100-2096     TMP-0100-2196

The kit assesses the affinity of compounds to phosphatidylcholine membranes. Movement through membranes is known as drug transport either as passive diffusion or active transport. Understanding how drugs interact with biological membranes is a prerequisite to an appreciation of their pharmacokinetics and pharmacodynamics.

While a drug’s size, it’s lipophilicity influences its ability to passively diffuse through membranes, diffusion is also influenced by the drug’s structure and in particular its structure-structure interactions with the membrane.

Moreover, increasing a drug’s lipophilicity is not necessarily increasing its propensity to traverse through cell membranes. In fact, the higher a drug’s affinity to the membranes, the more likely it is to enter the membrane and not come out again. That means that drug can get effectively trapped in the membranes – a phenomenon well known as brain tissue binding or microsomal binding. This also has toxicological consequences as the compound accumulates the bodies tissues.     TMP-0400-1308     TMP-0400-2096

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