Elacridar (GF120918) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
IC50&Target
P-glycoprotein (Pgp), BCRP
体外研究
Elacridar inhibits P-glycoprotein (P-gp) labeling by [H]azidopine with a IC50 of 0.16 μM. In Caki-1 and ACHN cells, elacridar (2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and SU 11248 lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells.
体内研究
Oral co-administration of elacridar (100 mg/kg, p.o.) and PF-02341066 increases the plasma and brain concentrations and brain-to-plasma ratios of PF-02341066 in wild-type mice, equaling the levels in Abcb1a/1b; Abcg2 mice. 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. In Mrp4(-/-) mice, elacridar fully inhibits P-gp mediated transport of SKF 104864A, without siginificant effects on Bcrp1-mediated transport.
分子式
C34H33N3O5
分子量
563.64
CAS号
143664-11-3
中文名称
依克立达
运输条件
Room temperature in continental US; may vary elsewhere.