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Plasma Stability

The measurement of the stability of a new chemical entity in a matrix such as plasma helps in identifying and understanding the lability of known structural moieties (e.g. amides, sulphonamide, esters, lactones, lactams to name a few) in molecules in the prioritisation of these for in vivo PK studies. High instability can result in aberrant PK results due to high clearance and short half-lives.  Species differences in plasma stability for molecules is not uncommon and should be determined.

Sygnature’s plasma stability assay measures the stability of molecules in plasma from either mouse, rat and human (please enquire about other species). The molecule to be tested and controls (positive and negative) are incubated with plasma for a defined period and the percent remaining and half-life determined.

Propantheline (human), Enalapril (mouse & rat), Vinpocetin (rat) and/or Benfluorex (human and rat) are included as positive control compounds. Pepstatin or Leupeptin are included as negative controls.

Protocol

Compound requirements 10mM DMSO, 50µL
Final DMSO concentration 1 %
Test Article Concentrations 1 μM
Incubation Time 0, 10, 20, 30, 60 and 120 min at 37°C
Test System Plasma
Analysis Method LC-MS/MS
Controls Propantheline (human), Enalapril (mouse & rat), Vinpocetin (rat) Benfluorex (human and rat) (positive controls)

Pepstatin, Leupeptin (negative control)

Data Delivery Plasma t1/2 (min) and percent compound remaining (%)

Results

Figure 1 Stability of compounds in mouse, rat and human plasma.

About Us

The DMPK & Physical Sciences department at Sygnature Discovery is dedicated to understanding and optimising the absorption, distribution, metabolism and excretion of drug candidates by working in close partnership with clients and other departments within Sygnature to provide successful optimisation strategies.

We have extensive know-how and expertise to provide well validated, state-of-the-art assays and a comprehensive applied consultancy service for interpretation of the in vitro ADME and in vivo PK data.

Our corporate vision is to accelerate the discovery of new medicines, from the laboratory into development to treat patients.

Our DMPK mission is to deliver tailored DMPK expertise through innovation, quality and commitment.

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