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Assays for ADME and Pharmacokinetics, and Toxicological Research for Drug Discovery and Development

Deutscher Platz 5b,
04103 Leipzig,
Fax Number

Sovicell provides assays for ADME and pharmacokinetics, and toxicological research for drug discovery and drug development.

Sovicell’s TRANSIL® assays can be used for assessing plasma protein binding and intestinal absorption, predicting the distribution volume, and assessing absorption across the blood-brain barrier as well as brain availability and neurotoxicity.

Smart dialysis systems

TRANSIL ready-to-use assay kits are smart dialysis systems that use an immobilised biological matrix with a very large surface area. This allows both rapid equilibration of dialysate binding and fast separation of the analyte from the matrix in downstream LC / MS / MS. As the assays do not require filter or dialysis membranes they avoid issues of unspecific binding to these filters and provide means to assess physical properties of both small molecules and peptides. Features include:

  • 2min incubation
  • Matrix free: down to 1/10 gradient duration in downstream LC / MS / MS
  • Ready-to-use: 96-well plates or plates of 12 tube units of eight tubes
  • Automation-friendly, and applicable to small molecules and peptides
  • Highly reproducible results due to smart dialysis technique

Brain absorption assay kit

Sovicell’s brain absorption kit is a ready-to-use assay kit that assesses how drug candidates pass across the blood-brain barrier, and estimates the binding of drugs to brain tissue. This allows the accurate prediction of drug candidates’ efficacy at receptors in the brain as well as the early prediction of side effects in the central nervous system.

The kit rapidly assesses drug candidates’ brain tissue binding, i.e. fu (brain) and its brain-to-plasma distribution coefficient to understand the free concentration of the drug in the brain. It classifies CNS compounds more accurately as measured by brain availability and brain membrane affinity (87% vs. PAMPA BBB 60%).

The kit determines the equilibrium distribution of drug compounds between blood and brain tissue protein binding kits (HSA, AGP and RSA), and quickly determines the binding of drugs to plasma binding protein – a true measurement of the free fraction of a drug candidate in plasma. Features include:

  • All natural brain lipids fully quality controlled
  • High reproducibility
  • Matrix free: down to 1/10 gradient duration in downstream LC / MS / MS
  • Brain free fraction (brain tissue binding) and brain-to-plasma distribution coefficient in less than 2hr processing time, including LC / MS / MS (12 compounds in six replicates)

Plasma protein binding kit

The TRANSIL plasma protein binding kit is a ready-to-use binding kit designed to assess the binding of drugs to plasma binding protein. It mimics the physiological condition of the major plasma protein human serum albumin (HSA) and α1-acid glycoprotein.

This kit is the most accurate method for strongly bound drugs, and the only method to assess binding in different plasma compositions. There are no issues due to plasma instability and all natural protein is fully quality controlled.

The kit has high reproducibility and is matrix free (down to 1/10 gradient duration in downstream LC / MS / MS). Protein binding data can be obtained in less than 2hr processing time, including LC / MS / MS (12 compounds in six replicates).

Intestinal absorption kit

The TRANSIL intestinal absorption kit is a ready-to-use kit designed for rapid assessment of drug candidates’ ability to cross the intestinal epithelium. The kit only requires the addition of drug candidates to the microtiter wells followed by a 2min incubation. The affinity of the drug candidate is a measurement of its passive transport in the gastrointestinal (GI) tract.

These kits predict the fraction absorbed, the permeability rate and the volume of distribution, and have strong correlation with in vivo tissue distribution data. They are matrix free (down to 1/10 gradient duration in downstream LC / MS / MS) and can obtain permeability data in less than 2hr processing time, including LC / MS / MS (12 compounds in six replicates).

High-protein binding assay

The TRANSIL high-protein binding assay is a variant of the erythrocyte partitioning. This assay is based on the partitioning of the test item between the plasma and membrane.

This assay utilises the observation that the membrane affinity of a compound in plasma divided by the membrane affinity of this compound in buffer equals the free fraction of the compound. Hence, this assay is concerned with estimating these membrane affinities, instead of measuring free fractions of drug in plasma. Features include:

  • Accurate protein binding data for small molecules and peptides
  • Discrimination of compounds with fu <1%
  • Works well with lipophilic compounds and peptides
  • No bias through unspecific binding
  • Complete high semi through-put assay scheme

Sovicell GmbH

Deutscher Platz 5b
04103 Leipzig

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