PharmTox

Home> Transporters>

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 (including polymorphisms and mutations) 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
ABCA1 ABCA1 human Cholesterol Cholesterol
ABCG1 ABCG1 human Cholesterol Cholesterol
GLUT1 SLC2A1 human D-Glucose Deoxy-D-Glucose
GLUT2 SLC2A2 human D-Glucose Deoxy-D-Glucose >3
GLUT5 SLC2A5 human D-Glucose Deoxy-D-Glucose >3
SGLT1 SLC5A1 human D-Glucose AMG >20
SGLT2 SLC5A2 human D-glucose AMG
SGLT1 SLC5A1 dog D-glucose AMG
DAT, Dopamine transporter SLC6A3 human Dopamine, Serotonin, ao Dopamine
SERT, Serotonin transporter SLC6A4 human Serotonin, Dopamine, ao Serotonin
LAT2 SLC7A8 (optional in combination with 4F2) human L-Alanine
NTCP SLC10A1 human Taurocholate, bile salts, DHEAS, Rosuvastatin, atorvastatin, pitavastatin, fluvastatin Taurocholate (TCA)
PEPT1 SLC15A1 human Gly-Sar (Glycyl-sarcosine) >20
PEPT2 SLC15A2 human Gly-Sar (Glycyl-sarcosine)
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 >3
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 >4
OCT3 SLC22A3 human Berberine, Epinephrine, Etilefrine, Histamine, Metformin, N-methylpyridinium, Norepinephrine, ao MDMA, Atropine, Berberine, Imipramine, Phenoxy-benzamine, Quinidine, Tetraethylammonium, ao Metformin >7
OCTN1 SLC22A4 human L-Carnitine >2
OCTN2 SLC22A5 human L-Carnitine >40
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 PAH
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
OAT4 SLC22A11 human
OAT5 SLC22A10 human
URAT1 SLC22A12 human Oxypurinol, Uric acid Benzbromarone, Fenofibric acid, Losartan, Morin, Pratosartan, Probenecid, Sulfinpyrazone, Telmisartan Uric acid
ENT4 SLC29A4 human
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
OATP1A2 SLCO1A1 human Taurocholic acid, Ursodeoxycholic acid, cholic acid, DHEAS, ao Statins, Ouabain, Imatinib, Fexofenadine, Atenolol, Testosterone, Naloxone, Quinidine, Rifampicin, ao Estrone sulfate
OATP1B1 SLCO1B1 available *1B, *4, *5, *15 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 >10




Home| Transporters| About us| Contact