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Transporters are the largest family of membrane proteins in human organism including members of solute carrier transporter and ATP-binding cassette transporter families. They play pivotal roles in the absorption, distribution and excretion of exogenous and endogenous molecules. Transporters are widely expressed in a variety of human tissues and are routinely evaluated during the process of drug development and approval. Currently, transporters are used as the therapeutic targets for the treatment of various diseases such as diabetes, major depression, hypertension, and constipation. Despite the steady growth of the field of transporter biology, we know very little about the endogenous substrates or physiological functions of more than half of the members in transporter superfamily. Therefore, understanding the interaction between the potential compounds and transporters in the early stage of drug development is critical for selecting candidates with desirable drug metabolism and safety profiles.

Creative Bioarray offers specialized transporter panels and customized transporter screening services enable you to identify novel transporter targeting compounds. Our transporter panels include FDA transporter screening panel, monoamine transporter models and many other cell models. We employ robust transporter uptake and inhibition assays to perform quick and efficient screening of new molecular entities (NMEs), and provide you results with good signal-to-background ratio and Z's scores.

Endpoints of Our Transporter Screening Services

  • P-gp inhibition
  • BCRP substrate identification
  • BCRP inhibition
  • SLC transporter substrate identification (OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1, MATE2-K, OATP1A2, OATP2B1, OAT2, OAT4, OCTN2, PEPT1, PEPT2, NTCP)
  • SLC transporter inhibition (OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1, MATE2-K, OATP1A2, OATP2B1, OAT2, OAT4, OCTN2, PEPT1, PEPT2, NTCP)
  • Preclinical hepatic Oatp uptake transporter substrate identification (rat Oatp1b2, dog Oatp1b4, and Cynomolgus monkey Oatp1b1)
  • Preclinical hepatic Oatp uptake transporter inhibition (rat Oatp1b2, dog Oatp1b4, and Cynomolgus monkey Oatp1b1)
  • BSEP inhibition
  • Other transporter assays available on request

Highlights of Our Transporter Screening

  • Cell-based assays providing functional characterization of compound activity
  • Coverage of key transporters
  • Availability of various panels
  • Short turn-around time
  • Customized screening project design

Technologies for Transporter Screening

  • Fluorescence
  • Radioactivity
  • Electrophysiology
  • Atomic absorption spectrophotometry (AAS)
  • Mass spectrometry

Transporter Screening    Figure 1. Transporters in intestinal epithelia, hepatocytes, kidney proximal tubules and brain capillary endothelial cells.

For more information on transporter drug discovery services, please contact us.

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