Uptake Transporter Characterized Cryopreserved Human Hepatocytes

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The uptake and efflux of a drug into and from hepatocytes can determine the rate at which the molecule is metabolized and eliminated from the body. The uptake transporters, including organic anion transporting polypeptides OATP1B1 (OATP2, OATP-C), OATP1B3 (OATP8) OATP2B1 (OATP-B), Na⁺-taurocholate co-transporting polypeptide (NTCP), organic cation transporter OCT1 and organic anion transporter OAT2, are expressed on the sinusoidal membrane of hepatocytes. These molecules are solute-linked carriers which use an electrochemical gradient of one solute to pump another molecule across the cell membranes and against its concentration gradient. Efflux transporters, multi-drug resistance protein (MDR1, P-gp, ABCB1), MDR3, BSEP (ABCB11, sP-gp), breast cancer resistance protein BCRP (ABCG2), and multi-drug resistance related protein MRP2 (ABCC2), are expressed on the canalicular membrane of hepatocytes and actively transport compounds into the bile. Other “efflux” transporters such as MRP1, 3 and 4 (ABCC1, 3 and 4) are expressed on the sinusoidal membrane of hepatocytes and therefore transport compounds from the cell into the blood.

Human hepatocytes in suspension can be used to evaluate active uptake of compounds into the cells. The uptake of estrone-3-sulfate, taurocholic acid, and 1-methyl-4-phenylpyridinium iodide (MPP+), substrates for OATP1B1, NTCP and OCT1, respectively, into cryopreserved human hepatocytes has been characterized with the method of Hallifax et. al., 2006.

If you are assessing how uptake transporters are affecting the metabolism of your compound, this is the product for you!

Download a Sample Uptake Transporter Characterized Hepatocyte Datasheet Here

Characterization Provided

• OATP Estrone-3-sulfate
• NTCP Taurocholic Acid
• OCT1 1-Methyl-4-phenylpyridinium lodine
• CYP2D6 Dextromethorphan O-demethylation
• CYP2E1 Chlorzoxazone 6-hydroxylation
• CYP3A4/5 Testosterone 6β-hydroxylation
• UGT Glucronidation of Methylumbelliferone

Donor information (age, ethnicity, gender, cause of death and infectious disease status)

Safety, Handling, and Storage

Cryopreserved hepatocytes should be stored in liquid nitrogen vapor (-160°C or colder). They should be thawed in accordance with our thawing protocol (PDF), which is shipped with your hepatocytes.

Upon thawing, cryopreserved human hepatocytes remain viable and may be used in suspension for short-term drug metabolism experiments (we recommend incubations no longer than 4 hours). When cryopreserved human hepatocytes are thawed, isolated, and suspended under appropriate conditions, they can be used to evaluate the metabolism of drug candidates.

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