New OATP2A1 uptake inhibition assay
December 21, 2011
SOLVO Biotechnology introduces the new OATP2A1 uptake inhibition assay with PGE2 as a probe substrate. The human OATP2A1 is a member of the Organic Anion Transporting Polipeptide (OATP/SLCO) family. This transporter is involved in the transport of prostaglandins (PGs), also known as prostaglandin transporter (PGT). It also transports latanoprost the antiglaucoma prostanoid. OATP2A1 is expressed in many tissues, including cell types that synthesize and release prostanoids, most importantly in the kidney, and play a fundamental role in context-dependent autocrine and paracrine signaling. Potent inhibitors of OATP2A1 transporter include furosemide, diclofenac, DIDs and Niflumic acid. In vitro data suggest that various clinically used COX inhibitors also can have differential impact on the function of the prostaglandin transporter OATP2A1 in human stomach and that these effects may contribute to differences in the gastrointestinal side effects of COX inhibitors. In our OATP2A1 uptake inhibition the probe substrate is Prostaglandin E2 (PGE2) and we use Diclofenac as reference inhibitor.Next entry: The new FDA Draft Guidance for Transporter DDI is out now
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