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Vesicular transport assays

Drug efflux transporters (ABC transporters) are transiently overexpressed in human embryonic kidney (HEK293) cells. Inside-out membrane vesicles are prepared from these cells and used for high-throughput applications. The transporters translocate various compounds into membrane vesicles in an ATP-dependent manner. Detection of the substrate inside the vesicles is possible with radiolabel, fluorescent or LC-MS detection. PharmTox delivers high quality large uniform batches with guaranteed transport ratios.
Transporters in the list below can be shipped directly after ordering. Transporters not in this list can be custom made within 2-3 months.

Transporter Gene name Species Substrates Inhibitors Test substrate AMP/ATP ratio
P-glycoprotein / MDR1 ABCB1 human convallatoxin, digoxin, N-methyl-quinidine (NMQ), colchicine, tacrolimus, quinidine, etoposide, doxorubicin ao verapamil, cyclosporin, tariquidar, PSC833, ao convallatoxin >5
BSEP, bile salt export pump ABCB11 human taurocholate, pravastatin, taurolitocholyl 3-sulfate, conjugated monovalent bile salts, ao cyclosporine A, rifampicin, glibenclamide ao TCA >20
BSEP, bile salt export pump ABCB11 rat TCA >10
BSEP, bile salt export pump ABCB11 dog TCA >10
BSEP, bile salt export pump ABCB11 cat TCA >10
MRP1, multidrug resistance associated protein 1 ABCC1 human E217bG, GSSG, saquinavir, ritonavir, methotrexate, daunorubicin, leukotrienes, prostaglandines, folic acid, ao 17b-Estradiol-D-17b-Glucuronide >5
MRP2, multidrug resistance associated protein 2 ABCC2 human CDCF, E217bG, methotrexate, etoposide, bilirubin conjugates, ao 5(6)-carboxy-2,'7'-dichlorofluorescein >20
MRP2, multidrug resistance associated protein 2 ABCC2 rat CDCF >20
MRP3, multidrug resistance associated protein 3 ABCC3 human E217bG, estradiol-17b-glucuronide, bile salts, methotrexate, vincristine, acetaminophen-glucuronide, ao 17b-Estradiol-D-17b-Glucuronide >15
MRP3, multidrug resistance associated protein 3 ABCC3 rat 17b-Estradiol-D-17b-Glucuronide >5
MRP4, multidrug resistance associated protein 4 ABCC4 human DHEAS, E217bG, taurocholic acid, urate, ritonavir, methotrexate, cAMP, ao Dehydroepiandrosterone sulfate >5
MRP4, multidrug resistance associated protein 4 ABCC4 rat p-aminohippuric acid >2
MRP5, multidrug resistance associated protein 5 ABCC5 human CDCF, methotraxate, cAMP, cGMP, folate, rouvastatin, ao 5(6)-carboxy-2,'7'-dichlorofluorescein >3
MRP8, multidrug resistance associated protein 8 ABCC11 human DHEAS, 5-fluoro-2'-deoxyuridine 5'-monophosphate (FdUMP), earwax, ao Dehydroepiandrosterone sulfate >3
BCRP ABCG2 human estrone-3-sulfate (E3S), methotrexate, irinotecan, pantoprazole, rosuvastatin, topotecan, chlorothiazide, ao Estrone-sulfate >10


Cellular transport assays

Human drug efflux and uptake transporters (ABC and SLC transporters) are transiently overexpressed in human embryonic kidney (HEK293) cells. The transport ratio is determined by comparing ctrl (mock transduced) with transporter transduced cells. The transporters translocate various compounds into or out of the cells. Detection of the substrate inside the cells is possible with radiolabel, fluorescent or LC-MS detection. PharmTox delivers high quality large uniform batches with guaranteed transport ratios.
Transporters not in this list can be custom made within 2-3 months.

Transporter Gene name Species Substrates Inhibitors Test substrate Transport ratio
OATP1B1 SLCO1B1 human Atorvastatin, Bilirubin, Bosentan, Bromsulphthalein (BSP), Cholate, Cholyl-glycylamido-fluorescein (CGamF), Cholyl taurine, Dehydroepiandrosterone sulfate, Estradiol-17beta-glucuronide, Estrone 3-sulfate, Fluo-3, Fluvastatin, Methotrexate, Olmesartan, Pravastatin, Rifampicin, Rosuvastatin, Tauroursodeoxycholate, Valsartan, ao Cyclosporine, Digoxin, Fenofibrate, Gemfibrozil, Lopinavir, MK-571, Troglitazone, ao 17b-Estradiol-D-17b-Glucuronide
OATP1B3 SLCO1B3 human Amantinin, Bilirubin, Bosentan, Bromsulphthalein (BSP), Cholecystokinin, Cholyl-glycylamido-fluorescein (CGamF), Digoxin, Estradiol-17beta-glucuronide, Estrone 3-sulfate, Fexofenadine, Fluo-3, Fluvastatin, Glycoursodeoxycholate, Methotrexate, Olmesartan, Paclitaxel, Rifampicin, Rosuvastatin, Taurocholate, Tauroursodeoxycholate, Telmisartan, Triiodothyronine, Valsartan, ao Cyclosporine, Darunavir, Lithocholate, Lopinavir, Mifepristone, MK-571, Paclitaxel, Penicillin G, Probenecid, Rifampicin, Ritonavir, ao 17b-Estradiol-D-17b-Glucuronide, TCA
OATP2B1 SLCO2B1 human Atorvastatin, Bosentan, Bromsulphthalein (BSP), Estrone 3-sulfate, Fexofenadine, Fluvastatin, Glyburide, Pitavastatin, Pravastatin, Rosuvastatin, Taurocholate, Telmisartan glucuronide, ao Cerivastatin, Cyclosporine, Estrone, Gemfibrozil, Indinavir, MK-571, Montelukast, Paclitaxel, Repaglinide, Rifampicin, Rifamycin SV, Ritonavir, Rosiglitazone, Saquinavir, Silibinin dihemisuccinate, Simvastatin, ao DHEAS
DAT, Dopamine transporter SLC6A3 human Dopamine, Serotonin, ao Dopamine
SERT, Serotonin transporter SLC6A4 human Serotonin, Dopamine, ao Serotonin
NTCP SLC10A1 human Taurocholate, bile salts, DHEAS, Rosuvastatin, atorvastatin, pitavastatin, fluvastatin Taurocholate (TCA)
OCT1 SLC22A1 human Acyclovir, Amiloride, Fenoterol, Furamidine, Ganciclovir, Glycopyrrolate, Ipratropium, Metformin, N-methylpyridinium, Prostaglandin E2, Ranitidine, Tetraethylammonium, ao MDMA, Atropine, Cimetidine, Clonidine, Diphenhydramine, Ketamine, Midazolam, Quinidine, Verapamil, ao Metformin
OCT2 SLC22A2 human ASP+, Amiloride, Cimetidine, Dopamine, Epinephrine, Metformin, N-methylpyridinium, Prostaglandin E2, Serotonin, Tetraethylammonium, ao MDMA, Atropine, Berberine, Cimetidine, Flurazepam, Imipramine, Quinine, Verapamil, ao Metformin
OCT3 SLC22A3 human Berberine, Epinephrine, Etilefrine, Histamine, Metformin, N-methylpyridinium, Norepinephrine, ao MDMA, Atropine, Berberine, Imipramine, Phenoxy-benzamine, Quinidine, Tetraethylammonium, ao Metformin
OAT1 SLC22A6 human 6-carboxyfluorescein, Adefovir, Cidofovir, Olmesartan, Para-aminohippurate, Prostaglandin E2, Uric acid Acetominophen, Adefovir, Betamipron, Chlorothiazide, Diclofenac, Furosemide, Ibuprofen, Indomethacin, Probenecid, ao CDCF
OAT2 SLC22A7 human Bumetanide, Cefoperazone, Cephalothin, Chlorothiazide, Diclofenac, Furosemide, Ibuprofen, Indomethacin, Ketoprofen, Mefenamic acid, Naproxen, Phenacetin, Piroxicam, Probenecid, Sulindac, ao MDMA, Atropine, Cimetidine, Clonidine, Decynium-22, Diphenhydramine, Furamidine, Memantine, Phencyclidine, Phenformin, Quinidine, Repaglinide, Verapamil, ao cGMP
OAT3 SLC22A8 human Bumetanide, Cefaclor, Cimetidine, Cortisol, Estrone-3-sulfate, Furosemide, Methotrexate, Pravastatin, Prostaglandin E2, Rosuvastatin, Tetracycline, Uric acid, ao Bumetanide, Candesartan, Ethacrynic acid, Furosemide, Ibuprofen, Naproxen, Olmesartan, Pratosartan, Quinapril, Sulindac, Valsartan, ao Estrone sulfate
URAT1 SLC22A12 human Oxypurinol, Uric acid Benzbromarone, Fenofibric acid, Losartan, Morin, Pratosartan, Probenecid, Sulfinpyrazone, Telmisartan Uric acid
MATE1 SLC47A1 human Cimetidine, Estrone sulfate, Ganciclovir, Metformin, Paraquat, Tetraethylammonium (TEA), ao Chloroquine, Cimetidine, Mixantrone, Pyrimethamine, Quinidine, Verapamil, oa Metformin
MATE2K SLC47A2 human Cimetidine, Estrone sulfate, Ganciclovir, Metformin, Tetraethylammonium (TEA), Topotecan, ao Cimetidine, Pyrimethamine, Quinidine, Verapamil, oa Metformin




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