Gibco™ Rat BCRP Vesicles

Description

Rat BCRP Vesicles are insect derived purified plasma membranes with inserted BCRP transport protein (Breast Cancer Resistance Protein, ABCG2). Our Rat BCRP Vesicles can be used to evaluate test compounds and drug interactions with BCRP in in vitro assays. BSEP is an ATP-binding cassette (ABC) transporter associated with multidrug resistance, which carries various anti-cancer drugs such as topotecan, methotrexate and mitoxantrone.

Use Rat BCRP Vesicles to:

• Investigate the transporter interactions of your drug candidates
• Assess potential for transporter-mediated drug-drug interactions
• Obtain high quality results with a large signal to noise ratios

Concept Behind ABC Transporter Vesicles

ABC transporter vesicles are easy-to-use, efficient reagents for early assessment of a drug candidate's substrate and drug interaction potential. While ABC transporters typically mediate the export of substrates out of cells, transporters expressed on these inside-out vesicles import substrates into the vesicles. It is therefore possible to quantitatively evaluate transport activity for your compound by determining the amount incorporated into the vesicles.

Clear and Reliable Results

Prepared from Sf9 cells which have been engineered to over-express specific ABC transporters, these 'inside-out' vesicles provide high levels of transporter activity with low background, giving you a clear signal if your compound is a substrate or inhibitor of a specific efflux transporter.

Transporter Vesicle Details

Rat BCRP Vesicles are part of a larger group of transporter vesicles known as ABC transporter vesicles. They are prepared from purified plasma membranes isolated from an insect cell system (Sf9 cells transfected with baculovirus) expressing BCRP. It is highly expressed in tumors like lung cancer and also in small intestinal epithelial cells, hepatic parenchymal cells, proximal renal tubule cells, and cerebrovascular endothelial cells. It is thought to be an important determinant of drug disposition, through its role in processes such as absorption at the small intestine, excretion into bile and urine, and transfer across the blood-brain barrier to the CNS.