Transporter Panel

Humanized and Knockout Mouse Models For In Vivo Applications

Drug transporters mediate uptake and extrusion of many compounds across biological barriers and can have profound effects on absorption, distribution metabolism, excretion, and toxicity (ADMET) of potential therapeutics. There is an increasing requirement to understand the role of such transporters on the ADMET characteristics of compounds in drug development, as highlighted by the recent white paper from the International Transporter Consortium (Nat Rev Drug Discov. 2010 Mar; 9(3):215-36). We offer a unique portfolio of transporter humanized and knockout mouse models which can be used for different in vivo applications.

Applications

Study the effect of transporter on blood-brain barrier penetration
Literature example: Semin Cancer Biol. 1997 Jun; 8(3):161-70.

Study the effect of transporters in bioavailability and clearance
Literature example: J Clin Invest. 2010 Aug; 120(8):2942-52.

Prediction of clinical drug-drug interactions
Literature example: J Clin Invest. 2010 Aug; 120(8):2942-52.

Determine the role of transporter in hyperbilirubinemia or other toxicity findings.
Literature example: J Clin Invest. 2012 Feb 1; 122(2):519-28.

Advantages

Use of pure inbred genetic background (either C57BL/6 or FVB). This will minimize variance between mice and increase reproducibility of results.
Corresponding mouse genes are deleted in the humanized models.
Pre-validation data available.

Available models

Transporter Panel
Knockouts	Humanized
Bcrp	MRP2
Mdr1a	OATP1B1
Mdr1a/b	OATP1B3
Mdr1a/b-Bcrp	OATP1B1-1B3
Mrp1
Oatp1a/1b