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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 (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 |
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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 |
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