Substrates for SLC transporters
Substrates of the various transporter isoforms were identified using in vitro transport studies of human or rodent isoforms or from in vivo studies using knockout mice or mutant rats. A number of substrates are provided. Not all substrates are included in this list.
| OATP1A2 | Sulfobromophthalein, BQ-123, cholic acid, dehydroepiandrosterone sulfate, deltophorin II, DPDPE, estrone-3-sulfate, fexofenadine, glycocholate, levofloxacin, methotrexate, microcystin-LR, ouabain, prostaglandin E2, rosuvastatin, saquinavir, taurocholate, thyroxine, triiodothyronine |
| OATP1B1 | Benzylpenicillin, bilirubin and its conjugates, bosentan, BQ-123, bromosulfophthalein, caspofungin, cerivastatin, cholic acid, dehydroepiandrosterone sulfate, DPDPE, estradiol 17β-glucuronide, estrone-3-sulfate, fluvastatin, glycocholate, irinotecan (SN38 metabolite), leukotriene C4, microcystin-LR, olmesartan, phalloidin, pravastatin, prostaglandin E2, rifampicin, rifampin, rosuvastatin, taurocholate, thromboxane B2, thyroxine, triiodothyronine, troglitazone sulfate, valsartan |
| OATP1B3 | Bilirubin conjugates, bosentan, sulfobromophthalein, BQ-123, cholecystokinin-8, dehydroepiandrosterone sulfate, deltorphin II, digoxin, DPDPE, docetaxel, estradiol 17β-glucuronide, fexofenadine, fluvastatin, glycocholate, irinotecan (SN38 metabolite), leukotriene C4, microcystin-LR, olmesartan, ouabain, paclitaxel, phalloidin, rifampicin, rifampin, rosuvastatin, taurocholate, telmisartan, thyroxine, triiodothyronine, valsartan |
| OCT1 | Acetylcholine, acyclovir, cimetidine, choline, dopamine, famotidine, ganciclovir, lamivudine, metformin, N-methylnicotinamide, 1-methyl-4-phenylpyridinium, quinine, ranitidine, serotonin, spermine, spermidine, tetraethylammonium, zalcitabine |
| OCT2 | Acetylcholine, amantadine, cimetidine, cisplatin, choline, dopamine, epinephrine, histamine, lamivudine, memantine, metformin, 1-methyl-4-phenylpyridinium, N-methylnicotinamide, norepinephrine, paraquat, prostaglandin E2, prostaglandin F2, quinine, ranitidine, serotonin, tetraethylammonium, zalcitabine |
| OCT3 | Atropine, dopamine, epinephrine, etilefrine, guanidine, histamine, 1-methyl-4-phenylpyridinium, tetraethylammonium |
| OCTN1 | l-Carnitine, ergothioneine, pyrilamine, quinidine, quinine, tetraethylammonium, verapamil |
| OCTN2 | l-Carnitine, cephaloridine, mildronate, pyrilamine, quinidine, spironolactone, tetraethylammonium, valproic acid, verapamil |
| OAT1 | Acetylsalicylate, acyclovir, adefovir, p-aminohippurate, cephaloridine, cidofovir, cimetidine, cyclic AMP and GMP, didanosine, edaravone sulfate, furosemide, ganciclovir, indoxyl sulfate, indomethacin, α-ketoglutarate, lamivudine, methotrexate, ochratoxin A, penicillin G, prostaglandins E2 and F2α, salicylate, stavudine, tetracycline, trifluridine, urate, zidovudine, zalcitabine |
| OAT2 | p-Aminohippurate, acetylsalicylate, allopurinol, bumetanide, cyclic AMP, dehydroepiandrosterone sulfate, estrone-3-sulfate, 5-fluorouracil, glutarate, α-ketoglutarate, methotrexate, paclitaxel, prostaglandins E2 and F2α, ochratoxin A, salicylate, tetracycline, valproic acid, zidovudine |
| OAT3 | Allopurinol, p-aminohippurate, benzylpenicillin, l-carnitine, cefazolin, cephaloridine, cholic acid, cimetidine, cortisol, dehydroepiandrosterone sulfate, edaravone sulfate, estrone-3-sulfate, famotidine, 5-fluorouracil, glutarate, glutathione, glycocholate, indoxyl sulfate, methotrexate, 6-mercaptopurine, ochratoxin A, pravastatin, prostaglandins E2 and F2α, rosuvastatin, taurocholate, tetracycline, urate, valacyclovir, zidovudine |
| OAT4 | p-Aminohippurate, dehydroepiandrosterone sulfate, estrone-3-sulfate, glutarate, indoxyl sulfate, ochratoxin A, tetracycline, zidovudine |
| PEPT1 | 5-Aminolevulinic acid, bestatin, cefadroxil, ceftibuten, cefixime, cephradine, cephalexin, glycylsarcosine |
| PEPT2 | 5-Aminolevulinic acid, bestatin, cefadroxil, glycylsarcosine, l-kyotorphin |
| CNT1 | Adenosine, cladribine, cytarabine, fialuridine, 5-fluorouridine, gemcitabine, stavudine, thymidine, uridine, zalcitabine, zidovudine |
| CNT2 | Adenosine, cladribine, clofarabine, cytidine, didanosine, fialuridine, 5-fluorouridine, formycin B, inosine, guanosine, ribavirin, tiazofurin, uridine |
| CNT3 | Adenosine, benzamide riboside, cladribine, clofarabine, cytarabine, cytidine, didanosine, fludarabine, 5-fluorouridine, gemcitabine, guanosine, inosine, 6-mercaptopurine, ribavirin, uridine, 6-thioguanine, tiazofurin, thymidine, zalcitabine, zebularine, zidovudine |
| ENT1 | Adenosine, cladribine, clofarabine, cytidine, fialuridine, gemcitabine, guanosine, ribavirin, thymidine, tiazofurin, uridine |
| ENT2 | Adenine, adenosine, clofarabine, cytidine, fialuridine, gemcitabine, guanine, guanosine, hypoxanthine, inosine, thymidine, tiazofurin, uridine |
| ENT3 | Adenine, adenosine, cladribine, fludarabine, guanosine, inosine, thymidine, uridine, zebularine, zidovudine |
| MATE1 | Acyclovir, cephalexin, cephradine, cimetidine, creatinine, estrone sulfate, ganciclovir, guanidine, 1-methyl-4-phenylpyridinium, metformin, oxaliplatin, paraquat, procainamide, tenofovir, tetraethylammonium, thiamine, topotecan |
| MATE2-K | Acyclovir, cimetidine, creatinine, estrone sulfate, ganciclovir, guanidine, metformin, 1-methyl-4-phenylpyridinium, N1-methylnicotinamide, oxaliplatin, procainamide, tetraethylammonium, thiamine, topotecan |