More Transporters
in Better Models


Optivia Delivers FDA Ready Reports

To order our services please call:
650-324-3177, extension 16
Toll Free: 888-OPTIVIA (888-678-4842)
Fax: 650-324-1855.




QUESTIONS?

Speak with one of our transporter specialists about your specific requirements to understand how we could help you and what kind of results you can expect.

CONTACT US:
888-OPTIVIA (888-678-4842)

Validated Transporter Assays from Optivia



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
and
The 9 EMA
Transporters
Transporter

  Gene

  Cell
  Model

  Probe
  Substrate

  Reference
  Inhibitor

P-gp
(MDR1)
FDA & EMA

ABCB1
MDCK-II
[3H]-digoxin verapamil

P-gp
(MDR1)
FDA & EMA

ABCB1
Caco-2
[3H]-digoxin verapamil

BCRP
FDA & EMA

ABCG2
Caco-2
[3H]-genistein chrysin

OAT1
FDA & EMA

SLC22A6
MDCK-II
[3H]-p-aminohippurate probenecid

OAT3
FDA & EMA

SLC22A8
MDCK-II
[3H]-estrone-3-sulfate probenecid

OATP1B1
FDA & EMA

SLCO1B1
MDCK-II
[3H]-estradiol-17ß-d-glucuronide rifampicin

OATP1B3
FDA & EMA

SLCO1B3
MDCK-II
[3H]-cholecystokinin-8 (CCK-8) rifampicin

OCT2
FDA & EMA

SLC22A2
MDCK-II
[14C]-metformin quinidine

OCT1
EMA

SLC22A1
MDCK-II
[14C]-metformin quinidine

BSEP
EMA

ABCB11
vesicle
[3H]-taurocholate rifampicin


Other Transporters

Transporter

  Gene

  Cell
  Model

  Probe
  Substrate

  Reference
  Inhibitor

OATP2B1

SLCO2B1
CHO
[3H]-estrone-3-sulfate bromosulfo-
phthalein

NTCP

SLC10A1
MDCK-II
[3H]-taurocholate glycocholate

CNT1

SLC28A1
MDCK-II
[3H]-uridine adenosine and gemcitabine

CNT2  New!

SLC28A2
MDCK-II
[3H]-uridine adenosine

PEPT1  New!

SLC15A1
MDCK-II
[3H]-GLY-SAR losartan and Ala-Glu

PEPT2  New!

SLC15A2
MDCK-II
[3H]-GLY-SAR losartan

OAT4  New!

SLC22A11
MDCK-II
[3H]-estrone-3-sulfate indomethacin

MRP2  New!

ABCC2
MDCK-II
[3H]-estradiol-17ß-d-glucuronide benzbromarone

MATE1  New!

SLC47A1
MDCK-II
[14C]-metformin cimetidine

MATE2-K  New!

SLC47A2
MDCK-II
[14C]-metformin cimetidine

TAUT1  New!

SLC6A6
MDCK-II
[3H]-GABA beta-alanine

SMVT  New!

SLC5A6
MDCK-II
[3H]-biotin
(Vitamin B7)
pantothenate (Vitamin B5)


Dual Transporter Models

Transporter

  Gene

  Cell
  Model

  Probe
  Substrate

  Reference
  Inhibitor

OCT1 / MATE1  New!

SLC22A1 / SLC47A1
MDCK-II
MPP+ cimetidine

OCT2 / MATE1  New!

SLC22A2 / SLC47A1
MDCK-II
[14C]-metformin cimetidine

OCT2 / MATE2-K  New!

SLC22A2 / SLC47A2
MDCK-II
[14C]-metformin cimetidine