hOAT1 (SLC22A6)

The human organic anion transporter 1 (OAT1; SLC22A6) is highly expressed at the basolateral membrane of proximal tubule cells in human kidneys. There OAT1 mediates the transport of numerous endogenous and exogenous compounds like antibiotics, diuretics, NSAID (non-steroidal anti-inflammatory drugs), antivirals, cytostatics and toxins. OAT1 facilitate the first step uptake at basolateral membrane of proximal tubule cells for renal secretion of a huge number of substrates. Therefore, the regulatory agencies decided that drugs eliminated significantly via the kidney have to be tested as potential inhibitors (substrates) for hOAT1.

Main localization:
Kidney
Transporter assay:
Uptake transporter assay (potential inhibitors or substrates)
Probe substrates:
p-Aminohippuric acid (PAH)
Probe inhibitors:
Probenecid, glibenclamide
Regulatory relevance:
FDA and EMA guidance
Important interacting drugs:
Adefovir, acyclovir, methotrexate, ochratoxin A, olmesartan, probenecid, bumetanide, diclofenac, fluvastatin, furosemide, ibuprofen
From other species:
rOat1, mOat1


Inhibition of hOAT1 mediated PAH uptake by different drugs (100 µM)
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