Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||41 mg/mL in DMSO|
Brain distribution and bioavailability of elacridar after different routes of administration in the mouse.
Sane R, et al. Drug Metab Dispos. 2012 Aug;40(8):1612-9. PMID: 22611067.
|Related P-gp Products|
Elacridar hydrochloride is a p-gp inhibitor.
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Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/mL in HeLa cell.
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
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