Elacridar hydrochloride is a p-glycoprotein (P-gp/ABCG1) inhibitor. Blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin and vincristine in CHRC5 cells. Also inhibits breast cancer resistance protein (BCRP/ABCG2). Orally active.
|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||DMSO 6 mg/mL (May need ultrasonic)|
5-HT3 receptor antagonists, a new approach in emesis: a review of ondansetron, granisetron and tropisetron.
Seynaeve, et al. Anticancer Drugs. 1991;2: 343. PMID: 1665723.
|Related P-gp Products|
Valspodar is a P-glycoprotein (P-gp) inhibitor widely used as overcoming multidrug resistance modulator.
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.
Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
Sinapine, an alkaloid derived from seeds of the cruciferous species, possess antioxidant and radio-protective activities, downregulats multi-drug resistance 1 (MDR1) expression.
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