Elacridar

Overview

Elacridar hydrochloride (GF120918A) 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. 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.

Application

Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Neurological Disease | P-glycoprotein

Product Information

• Catalog No.: B0084-311800
• CAS No.: 143664-11-3
• Molecular Formula: C34H33N3O5
• Molecular Weight: 563.654
• Purity: 98%

Source

Original product source