PortaCellTec biosciences GmbH

Inhibition studies


To determine the inhibitory potential of a test item the intracellular accumulation of the labeled probe substrate is performed in the absence or presence of increasing concentrations of the test item.
Experience has shown that a two-step procedure is recommendable:

First Step

Two point Inhibition: Inhibition of transporter-mediated uptake of a probe substrate by two different concentrations of a test item.

 

Two point Inhibition


Second Step
Determination of IC50 value: Concentration dependent inhibition of a probe substrate by a test item and determination of the half-maximal inhibition value (IC50). .

IC50 determination

 

Alternative Second Step
Determination of the inhibition character (Ki value): Dixon Plot analysis to determine competitive or non-competitive inhibition.

 

 

Service


Drug transporter assays

  Study design

  Assay performance

  Inhibition studies

  Substrate studies


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PortaCellTec Biosciences GmbH

 

Weender Landstraße 94 -108
37075 Göttingen
Tel : +49 551 309 66440
E-mail: PortaCellTec



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News

New validated products:

  • mNtcp
  • mOct1

Events

3rd German Pharm-Tox Summit
Göttingen, Germany
26 February - 1 March 2018


Pharmaforum
Saarbrücken, Germany
8 March 2018

 

AAPS Workshop
Virginia, USA
16 - 18 April 2018

 

20th Barrier- and
Transporter-Meeting

Bad Herrenalb, Germany
7 - 9 May 2018

Greifswalder Transporttage 2018
Greifswald, Germany
7 - 9 September 2018

 


Guidance for Industry (FDA and EMA)

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