Table 1.

Substrate classes of human OATPs

OATP	Endogenous substrates	Xenobiotic substrates	Model substrates
OATP1A2	bile salts, bilirubin, steroid hormone metabolites, thyroid hormones and metabolites,	liver function markers, β-blockers, statins, antiviral drugs, antibiotics, mushroom toxins, neuropeptides, anticancer drugs	Bromosulfophthalein Estrone-3-sulfate Fexofenadine
OATP1B1	bile salts, bilirubin, steroid hormone metabolites, thyroid hormones and metabolites, inflammatory mediators	liver function markers, mushroom toxins, statins, sartanes, antibiotics, antiviral drugs, anticancer drugs	Bromosulfophthalein Estradiol-17β-glucuronide Estrone-3-sulfate Pitavastatin Atorvastatin Pravastatin Rosuvastatin Valsartan
OATP1B3	bile salts, bilirubin, steroid hormone metabolites, thyroid hormones, inflammatory mediators	liver function markers, mushroom toxins, statins, sartanes, antibiotics, antiviral drugs, anticancer drugs, peptides	Bromosulfophthalein Cholecystokinin octapeptide Estradiol-17β-glucuronide Valsartan
OATP1C1	thyroid hormones and metabolites, steroid hormone metabolites	liver function markers	Thyroxine
OATP2A1	inflammatory mediators		Prostaglandines (PGE1, PGE2, PGE2α)
OATP2B1	steroid hormone metabolites, inflammatory mediators, thyroid hormones	liver function markers, statins,	Bromosulfophthalein Estron-3-sulfate
OATP3A1	steroid hormone metabolites, inflammatory mediators, thyroid hormones		PGE1 PGE2
OATP4A1	bile salts, steroid hormone metabolites, thyroid hormones,		Triiodothyronine Taurocholate
OATP4C1	bile salts, steroid hormone metabolites, thyroid hormones		Estrone-3-sulfate Digoxin

For a detailed recommendation of OATP probe substrates and inhibitors, please refer to: (Brouwer et al., 2013)