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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 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|
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
Tariquidar (XR9576) is a selective, highly efficacious third generation P-glycoprotein (P-gp) inhibitor.
The pipecolinate derivative Biricodar (VX-710, Incel) is a clinically applicable modulator of P-glycoprotein (Pgp) with potential chemosensitizing activity.
LY335979 (Zosuquidar trihydrochloride) is a selective Pgp (P-glycoprotein) inhibitor with a Ki of 59 nM.
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