CP-100356 hydrochloride (E5985-GRP)

CP-100356 hydrochloride is an orally active dual inhibitor of MDR1 (P-gp) and BCRP, with IC50 of ∼0.5 µM for MDR1-mediated calcein-AM transport inhibition and ∼1.5 µM for BCRP-mediated prazosin transport inhibition. It is also a weak inhibitor of OATP1B1 (IC50 ∼ 66 µM).