Tariquidar is a highly selective, potent non-competitive inhibitor of P-glycoprotein. P-glycoprotein actively transports structurally unrelated compounds out of cells, conferring the multidrug resistance phenotype in cancer. P-gp is also expressed in normal tissues like blood brain barrier, gastrointestinal track, liver, spleen and kidney. Tariquidar profoundly inhibited P-glycoprotein in lymphocytes by 93.7% (95% confidence interval, 92.0-95.3%). Tariquidar (XR9576) inhibits the ATPase activity of P-glycoprotein, suggesting that the modulating effect is derived from both inhibition of substrate binding and inhibition of ATP hydrolysis or each of them.
|Cell lines||HEK 293 cells|
|Preparation method||A sample of the isolated histidine-tagged P-gp was mixed with an equal volume of 10 mg/ml of sheep brain phosphatidylethanolamine that had been washed and suspended in TBS. ATPase activity was measured in the presence of various concentrations of tariquidar.|
|Concentrations||0.25 µM, 0.5 µM, 1 µM,|
|Incubation time||24 h|
|Animal models||Balb/C mice|
|Formulation||water with 5% glucose|
|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.
Reversal of multidrug resistance by co-delivery of tariquidar (XR9576) and paclitaxel using long-circulating liposomes.
Patel NR, et al. Int J Pharm. 2011 Sep 15;416(1):296-9. PMID: 21703341.
|Related P-gp Products|
Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
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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