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Elacridar

CAS No. : 143664-11-3

MCE 站：Elacridar

产品活性：Elacridar (GF120918) 是一种有效的 P-糖蛋白 (P-glycoprotein) 和 BCRP 的抑制剂。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P-glycoprotein  |  BCRP

In Vitro: Elacridar inhibits P-glycoprotein (P-gp) labeling by [³H]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.

In Vivo: 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.

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