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BSEPcyte

BSEPcyte™ is a patented assay (United States patent number 9,772,325) that offers significant advantages over bile salt export pump (BSEP) assays that use membrane vesicle preparations. BSEPcyte™ is a physiologically relevant hepatocyte-based platform that measures test agent inhibition of BSEP or Bsep, provides cross-species comparisons, and offers the ability to investigate the effect of in situ drug metabolism on inhibition; the assay is run without radioactive reagents.

BSEPcyte™ employs a 96-well plate format with liquid chromatography-mass spectrometry quantification. The assay is accurate, reproducible, sensitive, and possesses a wide dynamic range. BSEPcyte™ was developed to be cost competitive and high-throughput.

BSEPcyte™ shows excellent correlation with drugs that cause human drug-induced liver injury (DILI) and BSEP inhibition. BSEPcyte™ is your assay to test BSEP inhibition and minimize the risk of unexpected DILI.

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Publications:

Aleo MD, Shah F, He K, Bonin PD, Rodrigues AD. Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4. PubMed PMID: 28437613.http://pubs.acs.org/doi/abs/10.1021/acs.chemrestox.7b00048

Yucha RW, He K, Shi Q, Cai L, Nakashita Y, Xia CQ, Liao M. In Vitro Drug-Induced Liver Injury Prediction: Criteria Optimization of Efflux Transporter IC50 and Physicochemical Properties. Toxicol Sci. 2017 Jun 1;157(2):487-499. doi:10.1093/toxsci/kfx060. PubMed PMID: 28369588. https://academic.oup.com/toxsci/article-abstract/157/2/487/3092345/In-Vitro-Drug-Induced-Liver-Injury-Prediction?redirectedFrom=fulltext

Zhang J, He K, Cai L, Chen YC, Yang Y, Shi Q, Woolf TF, Ge W, Guo L, Borlak J, Tong W. Inhibition of bile salt transport by drugs associated with liver injury in primary hepatocytes from human, monkey, dog, rat, and mouse. Chem Biol Interact. 2016 Mar 19. pii: S0009-2797(16)30089-8. doi:10.1016/j.cbi.2016.03.019. [Epub ahead of print] PubMed PMID: 27000539.http://www.sciencedirect.com/science/article/pii/S0009279716300898

Cheng Y, Woolf TF, Gan J, He K. In vitro model systems to investigate bile salt export pump (BSEP) activity and drug interactions: A review. Chem Biol Interact. 2015 Dec 10. pii: S0009-2797(15)30131-9. doi: 10.1016/j.cbi.2015.11.029. [Epub ahead of print] PubMed PMID: 26683212.http://www.sciencedirect.com/science/article/pii/S0009279715301319

 


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