Vesicle Kits

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Tackle your drug-drug interaction and substrate studies with our Vesicular Transport Assays

Human drug efflux transporters (ABC transporters) are transiently overexpressed in human embryonic kidney (HEK293) cells. Inside-out membrane vesicles are prepared from these HEK293 cells and used for high-throughput applications. The transporters translocate substrates into membrane vesicles in an ATP-dependent manner. Detection of the substrate inside the vesicles is possible with radiolabel, fluorescence, or LC-MS detection. Cell4Pharma delivers high quality large uniform batches with guaranteed transport ratios. Each vesicle kit contains the following materials for 100 reactions:

  • Membrane vesicles
  • AMP solution
  • ATP solution
  • Assay buffer
  • Stop/Wash buffer

Explore our novel fluorescent substrate FluoPgp!

Complete list of all available transporters
Vesicular Transport Assays One-pager (PDF)
Vesicular Transport Assay General Protocol

Our vesicles have an unmet dynamic range compared to others in the market.

PgP

Inside-out membrane vesicles isolated from HEK293 cells. PgP vesicles with an ATP/AMP ratio >5 are readily available from Cell4Pharma. PgP mediated convallatoxin (digoxin analogue) transport:

Name: MDR1, multidrug resistance protein 1, permeability glycoprotein, P-gp, ATP-binding cassette sub-family B member 1, ABCB1.

Diseases: – .

PgP substrates: FluoPgp, N-methyl-quinidine (NMQ), convallatoxin, digoxin, colchicine, tacrolimus, quinidine, etoposide, doxorubicin, etc. PgP is present in: Intestine, liver, kidney, blood-brain barrier, many tumor cells.

For ordering information or product quotes please contact us here.
Data sheet MDR1

BSEP

Inside-out membrane vesicles isolated from HEK293 cells. BSEP vesicles with an ATP/AMP ratio >10 are readily available from Cell4Pharma.

BSEP mediated TCA transport:

Name: BSEP, Bile Salt Export Pump, ATP-binding cassette sub-family B member 11, ABCB11.
Diseases: inherited and drug-induced cholestasis.
BSEP substrates: taurocholate, pravastatin, taurolitocholyl 3-sulfate, conjugated monovalent bile salts.
BSEP is present in: canalicular plasma membrane of hepatocytes.

For ordering information or product quotes please contact us here.
Data sheet BSEP

MRP1

Inside-out membrane vesicles isolated from HEK293 cells. MRP1 vesicles with an ATP/AMP ratio >5 are readily available from Cell4Pharma.

MRP1 mediated E217bG transport:

Name: MRP1, multidrug resistance associated protein 1, ATP-binding cassette sub-family C member 1, ABCC1.
Diseases: – .
MRP1 substrates: E217bG, GSSG, saquinavir, ritonavir, methotrexate, daunorubicin, leukotrienes, prostaglandines, folic acid, etc.
MRP1 is present in: lung, testis, kidney, blood-brain barrier, skeletal and cardiac muscles, placenta, and macrophages.

For ordering information or product quotes please contact us here.
Data sheet MRP1

MRP2

Inside-out membrane vesicles isolated from HEK293 cells. MRP2 vesicles with an ATP/AMP ratio >20 are readily available from Cell4Pharma.

MRP2 mediated CDCF transport:

Name: MRP2, multidrug resistance associated protein 2, cMOAT, canalicular multispecific organic anion transporter, ATP-binding cassette sub-family C member 2, ABCC2.
Diseases: Dubin-Johnson syndrome.
MRP2 substrates: CDCF, E217bG, methotrexate, etoposide, bilirubin conjugates, etc.
MRP2 is present in: liver, kidney, blood-brain-barrier, intestine, colon, bronchi and placenta.

For ordering information or product quotes please contact us here.
Data sheet MRP2

MRP3

Inside-out membrane vesicles isolated from HEK293 cells. MRP3 vesicles with an ATP/AMP ratio >10 are readily available from Cell4Pharma.

MRP3 mediated E217bG transport:

Name: MRP3, multidrug resistance associated protein 3, ATP-binding cassette sub-family C member 3, ABCC3.
Diseases: – .
MRP3 substrates: E217bG, estradiol-17b-glucuronide, bile salts, methotrexate, vincristine, acetaminophen-glucuronide, etc.
MRP3 is present in: liver, gallbladder, pancreas, intestine, colon, kidney, spleen and adrenal cortex .

For ordering information or product quotes please contact us here.
Data sheet MRP3

MRP4

Inside-out membrane vesicles isolated from HEK293 cells. MRP4 vesicles with an ATP/AMP ratio >5 are readily available from Cell4Pharma.

MRP4 mediated DHEAS transport:

Name: MRP4, multidrug resistance associated protein 4, MOATB, ATP-binding cassette sub-family C member 4, ABCC4.
Diseases: – .
MRP4 substrates: DHEAS, E217bG, taurocholic acid, urate, ritonavir, methotrexate, cAMP, etc.
MRP4 is present in: kidney, prostate, liver, pancreas and choroid plexus basolaterally and brain capillary endothelial cells apically.

For ordering information or product quotes please contact us here.
Data sheet MRP4

MRP5

Inside-out membrane vesicles isolated from HEK293 cells. MRP5 vesicles with an ATP/AMP ratio >3 are readily available from Cell4Pharma.

MRP5 mediated CDCF transport:

Name: MRP5, multidrug resistance associated protein 5, MOATC, ATP-binding cassette sub-family C member 5, ABCC5.
Diseases: – .
MRP5 substrates: CDCF, methotrexate, cAMP, cGMP, folate, rosuvastatin, etc.
MRP5 is present in: liver, lung, urethra, blood-brain-barrier, choroid plexus, skeletal muscle, heart, and placenta.

For ordering information or product quotes please contact us here.
Data sheet MRP5

MRP8

Inside-out membrane vesicles isolated from HEK293 cells. MRP8 vesicles with an ATP/AMP ratio >3 are readily available from Cell4Pharma.

MRP8 mediated DHEAS transport:

Name: MRP8, ATP-binding cassette sub-family C member 11, ABCC11.
Diseases: – .
MRP8 substrates: DHEAS, 5-fluoro-2′-deoxyuridine 5′-monophosphate (FdUMP), earwax, etc.
MRP8 is present in: brain, breasts, lungs, liver, kidney, placenta, prostate, testes, gastrointestinal tract tissues, gastric mucosa, and apocrine glands.

For ordering information or product quotes please contact us here.
Data sheet MRP8

BCRP

Inside-out membrane vesicles isolated from HEK293 cells. BCRP vesicles with an ATP/AMP ratio >10 are readily available from Cell4Pharma.

BCRP mediated E1S transport:

Name: BCRP, breast cancer resistance protein, ATP-binding cassette sub-family G member 2, ABCG2.
Diseases: – .
BCRP substrates: E1S, estrone-3-sulfate, methotrexate, irinotecan, pantoprazole, rosuvastatin, topotecan, chlorothiazide etc.
BCRP is present in: placenta, stem cells, prostate, small intestine, brain, colon, liver, mammary gland and kidney.

For ordering information or product quotes please contact us here.
Data sheet BCRP

Our vesicles have an unmet dynamic range compared to others in the market.

PGP

Inside-out membrane vesicles isolated from HEK293 cells. PgP vesicles with an ATP/AMP ratio >5 are readily available from Cell4Pharma. PgP mediated convallatoxin (digoxin analogue) transport:

Name: MDR1, multidrug resistance protein 1, permeability glycoprotein, P-gp, ATP-binding cassette sub-family B member 1, ABCB1.

Diseases: – .

PgP substrates: convallatoxin, digoxin, N-methyl-quinidine (NMQ), colchicine, tacrolimus, quinidine, etoposide, doxorubicin, etc. PgP is present in: Intestine, liver, kidney, blood-brain barrier, many tumor cells.

In stock: human Pgp.
Available: mouse and rat Pgp.

For ordering information or product quotes please contact us here.

BSEP

Inside-out membrane vesicles isolated from HEK293 cells. BSEP vesicles with an ATP/AMP ratio >10 are readily available from Cell4Pharma.

BSEP mediated TCA transport:

Name: BSEP, Bile Salt Export Pump, ATP-binding cassette sub-family B member 11, ABCB11.
Diseases: inherited and drug-induced cholestasis.
BSEP substrates: taurocholate, pravastatin, taurolitocholyl 3-sulfate, conjugated monovalent bile salts.
BSEP is present in: canalicular plasma membrane of hepatocytes.

In stock: human, cat, and dog BSEP.
Available: mouse and rat BSEP.

For ordering information or product quotes please contact us here.

MRP1

Inside-out membrane vesicles isolated from HEK293 cells. MRP1 vesicles with an ATP/AMP ratio >5 are readily available from Cell4Pharma.

MRP1 mediated E217bG transport:

Name: MRP1, multidrug resistance associated protein 1, ATP-binding cassette sub-family C member 1, ABCC1.
Diseases: – .
MRP1 substrates: E217bG, GSSG, saquinavir, ritonavir, methotrexate, daunorubicin, leukotrienes, prostaglandines, folic acid, etc.
MRP1 is present in: lung, testis, kidney, blood-brain barrier, skeletal and cardiac muscles, placenta, and macrophages.

In stock: human MRP1.
Available: mouse and rat MRP1.

For ordering information or product quotes please contact us here.

MRP2

Inside-out membrane vesicles isolated from HEK293 cells. MRP2 vesicles with an ATP/AMP ratio >20 are readily available from Cell4Pharma.

MRP2 mediated CDCF transport:

Name: MRP2, multidrug resistance associated protein 2, cMOAT, canalicular multispecific organic anion transporter, ATP-binding cassette sub-family C member 2, ABCC2.
Diseases: Dubin-Johnson syndrome.
MRP2 substrates: CDCF, E217bG, methotrexate, etoposide, bilirubin conjugates, etc.
MRP2 is present in: liver, kidney, blood-brain-barrier, intestine, colon, bronchi and placenta.

In stock: human MRP2.
Available: mouse and rat MRP2.

For ordering information or product quotes please contact us here.

MRP3

Inside-out membrane vesicles isolated from HEK293 cells. MRP3 vesicles with an ATP/AMP ratio >10 are readily available from Cell4Pharma.

MRP3 mediated E217bG transport:

Name: MRP3, multidrug resistance associated protein 3, ATP-binding cassette sub-family C member 3, ABCC3.
Diseases: – .
MRP3 substrates: E217bG, estradiol-17b-glucuronide, bile salts, methotrexate, vincristine, acetaminophen-glucuronide, etc.
MRP3 is present in: liver, gallbladder, pancreas, intestine, colon, kidney, spleen and adrenal cortex .

In stock: human MRP3.
Available: mouse and rat MRP3.

For ordering information or product quotes please contact us here.

MRP4

Inside-out membrane vesicles isolated from HEK293 cells. MRP4 vesicles with an ATP/AMP ratio >5 are readily available from Cell4Pharma.

MRP4 mediated DHEAS transport:

Name: MRP4, multidrug resistance associated protein 4, MOATB, ATP-binding cassette sub-family C member 4, ABCC4.
Diseases: – .
MRP4 substrates: DHEAS, E217bG, taurocholic acid, urate, ritonavir, methotrexate, cAMP, etc.
MRP4 is present in: kidney, prostate, liver, pancreas and choroid plexus basolaterally and brain capillary endothelial cells apically.

In stock: human MRP4.
Available: mouse and rat MRP4.

For ordering information or product quotes please contact us here.

MRP5

Inside-out membrane vesicles isolated from HEK293 cells. MRP5 vesicles with an ATP/AMP ratio >3 are readily available from Cell4Pharma.

MRP5 mediated CDCF transport:

Name: MRP5, multidrug resistance associated protein 5, MOATC, ATP-binding cassette sub-family C member 5, ABCC5.
Diseases: – .
MRP5 substrates: CDCF, methotraxate, cAMP, cGMP, folate, rouvastatin, etc.
MRP5 is present in: liver, lung, urethra, blood-brain-barrier, choroid plexus, skeletal muscle, heart, and placenta.

In stock: human MRP5.
Available: mouse and rat MRP5.

For ordering information or product quotes please contact us here.

MRP8

Inside-out membrane vesicles isolated from HEK293 cells. MRP8 vesicles with an ATP/AMP ratio >3 are readily available from Cell4Pharma.

MRP8 mediated DHEAS transport:

Name: MRP8, ATP-binding cassette sub-family C member 11, ABCC11.
Diseases: – .
MRP8 substrates: DHEAS, 5-fluoro-2′-deoxyuridine 5′-monophosphate (FdUMP), earwax, etc.
MRP8 is present in: brain, breasts, lungs, liver, kidney, placenta, prostate, testes, gastrointestinal tract tissues, gastric mucosa, and apocrine glands.

In stock: human MRP8.
Available: mouse and rat MRP8.

For ordering information or product quotes please contact us here.

BCRP

Inside-out membrane vesicles isolated from HEK293 cells. BCRP vesicles with an ATP/AMP ratio >10 are readily available from Cell4Pharma.

BCRP mediated E1S transport:

Name: BCRP, breast cancer resistance protein, ATP-binding cassette sub-family G member 2, ABCG2.
Diseases: – .
BCRP substrates: E1S, estrone-3-sulfate, methotrexate, irinotecan, pantoprazole, rosuvastatin, topotecan, chlorothiazide etc.
BCRP is present in: placenta, stem cells, prostate, small intestine, brain, colon, liver, mammary gland and kidney.

In stock: human BCRP.
Available: mouse and rat BCRP.

For ordering information or product quotes please contact us here.

Membrane vesicles

Cell4Pharma 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 upon request.

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

Cell4Pharma delivers high quality large uniform batches with guaranteed transport ratios. Membrane vesicles of transporters in the list below are available. Transporters not in this list (e.g. mouse or rat derivatives and genes including polymorphisms and mutations) can be custom made upon request.

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

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. Cell4Pharma 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 months.

Vesicular Transport Assays List

Cellular Transport Assays

Cellular Transport Assays are under development with promising data. Current development includes transferring ready to use product to our customers upon request. Alternatively, contract research activities are available upon request.

Cellular Transport Assays List

Our vesicles have an unmet dynamic range.

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