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Molecular structure and tissue distribution
OATP1A2 (formerly termed OATP or OATP-A) was the first member of the human OATP family to be cloned and functionally characterized. The human SLCO1A2 gene (NCBI Accession ID: NM_021094) is located on chromosome 12p12. The human OATP1A2 protein consists of 670 amino acids and is highly expressed in brain, but also in kidney and liver. It is suggested that hOATP1A2 plays an important role at the blood-brain barrier, where it can transport hormones and drugs.

Interaction of OATP1A2 with endogenous compounds and drugs

OATP1A2 transports bile salts, steroid hormones and their conjugates, thyroid hormones as well as some organic cations like N-methyl-quinidine (Km = 26 µM). Drug substrates of hOATP1A2 are e.g. fexofenadine (Km = 6 µM), tauroursodeoxycholate (Km = 19 µM) and ouabain (Km = 5.5 µM).
Several studies have identified genetic variations within the SLCO1A2 gene, some of these variants showed altered uptake in vitro.



New validated products:

  • MRP2
  • roct1


2nd German Pharm-Tox Summit
Heidelberg, Germany
March 06-09, 2017

19th Barrier- and

Bad Herrenalb, Germany
May 15-17, 2017

14th European ISSX Meeting
Köln, Germany

June 26- 29, 2017

2nd Symposium on Transporters in Drug Discovery
London, UK
May 15-16, 2017

Münster Transporttage 2017
Münster, Germany
October 21 – 22, 2017


Guidance for Industry (FDA and EMA)