Elacridar

143664-11-3

C34H33N3O5

DMSO : 5 mg/mL (8.87 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Membrane Transporter/Ion Channel; Membrane Transporter/Ion Channel

Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor. IC50 & Target: P-glycoprotein (Pgp), BCRP^[1] In Vitro: Elacridar inhibits P-glycoprotein (P-gp) labeling by [³H]azidopine with a IC₅₀ of 0.16 uM^[2]. In Caki-1 and ACHN cells, elacridar (2.5 uM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and sunitinib lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells^[3]. In Vivo: Oral co-administration of elacridar (100 mg/kg, p.o.) and crizotinib increases the plasma and brain concentrations and brain-to-plasma ratios of crizotinib in wild-type mice, equaling the levels in Abcb1a/1b; Abcg2^-/- mice^[1]. In friend leukemia virus stain B mice, the brain-to-plasm partition coefficient (Kp, brain) of elacridar is 0.82, 0.43, and 4.31 after intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg) treatment, respectively^[4]. In Mrp4(-/-) mice, elacridar fully inhibits P-gp mediated transport of topotecan, without siginificant effects on Bcrp1-mediated transport^[5].