依克立达
CAS号 | 143664-11-3 | 货号 | BCP05709 |
中文名 | 依克立达 | ||
英文名 | Elacridar | ||
中文别名 | |||
英文别名 | GF120918; GF-120918; GF 120918; GW 0918;GW-0918;GW0918; GG918;GG 918;GG-918; GF-120918; GF 120918; | ||
分子式 | C34H33N3O5 | 分子量 | 563.64 |
生物活性 | Elacridar is a P-glycoprotein (P-gp) inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects. | ||
信号通路 | Ion Channel/Membrane Transporter Neuro Signaling Pathway | ||
靶 点 | P glycoprotein BCRP |
结构式
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