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In vitro transporter inhibition studies are designed to determine if the investigational drug is an inhibitor of a transporter. Organic cation transporters (OCT) are expressed in the kidney, liver, and intestine, predominantly transport hydrophilic, low-molecular-weight organic cations. Measurement of transport for the known probe substrates of 1-methyl-4-phenylpyridinium (MPP+) and metformin by using LC-MS method can provide the in vitro indicator of OCT1 and OCT2 activity, respectively, for the inhibition assessment.
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