More Transporters
in Better Models
Optivia transporter assays measure functional transport of a substrate in a polarized mammalian cell. Inhibition assays monitor the transport of a marker substrate and substrate transport assays measure transport of your compound.
Optivia has both efflux transporter assays and uptake transporter assays, including the 7 FDA and 9 EMA transporters. Additionally, we offer other transporters with importance for DMPK, toxicology and pharmacology. Optivia also provides dual transporter models with clinical relevance.
Optivia assays are validated with both probe substrates and inhibitors and must meet criteria for reproducibility.
The 7 FDA | ||||
|---|---|---|---|---|
Transporter |
Gene |
Cell Model |
Probe |
Reference Inhibitor |
|
ABCB1 |
MDCK-II |
[3H]-digoxin | verapamil |
|
ABCB1 |
Caco-2 |
[3H]-digoxin | verapamil |
|
ABCG2 |
Caco-2 |
[3H]-genistein | chrysin |
|
SLC22A6 |
MDCK-II |
[3H]-p-aminohippurate | probenecid |
|
SLC22A8 |
MDCK-II |
[3H]-estrone-3-sulfate | probenecid |
|
SLCO1B1 |
MDCK-II |
[3H]-estradiol-17ß-d-glucuronide | rifampicin |
|
SLCO1B3 |
MDCK-II |
[3H]-cholecystokinin-8 (CCK-8) | rifampicin |
|
SLC22A2 |
MDCK-II |
[14C]-metformin | quinidine |
|
SLC22A1 |
MDCK-II |
[14C]-metformin | quinidine |
|
ABCB11 |
vesicle |
[3H]-taurocholate | rifampicin |
|
|
||||
| ||||
Transporter |
Gene |
Cell Model |
Probe |
Reference Inhibitor |
SLCO2B1 |
CHO |
[3H]-estrone-3-sulfate | bromosulfo- phthalein |
SLC10A1 |
MDCK-II |
[3H]-taurocholate | glycocholate | |
SLC28A1 |
MDCK-II |
[3H]-uridine | adenosine and gemcitabine | |
|
SLC28A2 |
MDCK-II |
[3H]-uridine | adenosine |
|
SLC15A1 |
MDCK-II |
[3H]-GLY-SAR | losartan and Ala-Glu |
|
SLC15A2 |
MDCK-II |
[3H]-GLY-SAR | losartan |
|
SLC22A11 |
MDCK-II |
[3H]-estrone-3-sulfate | indomethacin |
|
ABCC2 |
MDCK-II |
[3H]-estradiol-17ß-d-glucuronide | benzbromarone |
|
SLC47A1 |
MDCK-II |
[14C]-metformin | cimetidine |
|
SLC47A2 |
MDCK-II |
[14C]-metformin | cimetidine |
|
SLC6A6 |
MDCK-II |
[3H]-GABA | beta-alanine |
|
SLC5A6 |
MDCK-II |
[3H]-biotin (Vitamin B7) |
pantothenate (Vitamin B5) |
|
| ||||
Transporter |
Gene |
Cell Model |
Probe |
Reference Inhibitor |
|
SLC22A1 / SLC47A1 |
MDCK-II |
MPP+ | cimetidine |
|
SLC22A2 / SLC47A1 |
MDCK-II |
[14C]-metformin | cimetidine |
|
SLC22A2 / SLC47A2 |
MDCK-II |
[14C]-metformin | cimetidine |
