[]依克立达_抗生素_生化试剂


有效期 3年
别名 依克立达;ELACRIDAR (GF120918);N-[4-[2-(6,7-二甲氧基-3,4-二氢-1H-异喹啉-2-基)乙基]苯基]-5-甲氧基-9-氧代-10H-吖啶-4-甲酰胺
英文名称 Elacridar
CAS 143664-11-3
分子式 C34H33N3O5
分子量 563.64292
储存条件 2-8℃
纯度 ≥98%
单位

Biological Activity:
Elacridar (GF120918; GW0918) is a P-glycoprotein 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.
Target: P-glycoprotein

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.

Solvent & Solubility: 10 mM in DMSO

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