OATP2B1 (SLCO2B1)


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OATP2B1 Transporter: SLCO2B1



About OATP2B1
The OATP2B1 transporter is an organic anion uptake transporter that is encoded by the SLCO2B1 gene. OATP2B1 is expressed in liver hepatocytes on the basal-lateral side of the sinusoidal membrane. Because it serves to bring substrates into the liver from the blood stream, OATP2B1 can mediate the hepatic elimination of these compounds.

OATP2B1 is also expressed on the apical side of intestinal enterocytes serving to facilitate the absorption of substrates.

OATP2B1 has also been reported to be in the blood brain barrier.

OATP2B1 Substrates
OATP2B1 substrates include statins, ezetimibe, prostaglandin E2 and talinolol.

OATP2B1 Inhibitors
OATP2B1 inhibitors include bromosulfophthalein, atorvastatin and gemfibrozil.

Optivia OATP2B1 Transporter Assays
Optivia offers OATP2B1 substrate and inhibition assays in CHO cells. We offer a wide range of studies including single concentration screens up to full kinetic studies to determine the IC50 for OATP2B1 inhibitors and Vmax, Km and/or IC50 for OATP2B1 substrates.

The probe substrate for the Optivia OATP2B1 assay is estrone-3-sulfate. Bromosulfophthalein is the reference inhibitor. These serve as the positive controls for the OATP2B1 substrate assays and the OATP2B1 inhibition assays, respectively.