206873-63-4

Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (K_d = 5.1 nM) and inhibits transport activity. It inhibits transport of vinblastine (Item No. 11762) and paclitaxel (Item No. 10461) in multidrug resistant CH^rB30 cells, increasing the steady state accumulation to non-P-glycoprotein-expressing multidrug sensitive cell levels (EC₅₀ = 487 nM). Tariquidar also enhances the distribution of its substrates, increasing the amount of substrate entering the CNS. When administered at doses of 2 and 6.25 mg/kg in mice in combination with the peripherally-restricted opioid loperamide, the latency to paw withdrawal in a hot plate assay increases, indicating that loperamide is transported into the CNS.

Tariquidar is a p-glycoprotein drug efflux pump inhibitor. Tariquidar inhibits the ATPase activity of P-glycoprotein, suggesting that the modulating effect is derived from the inhibition of substrate binding, inhibition of ATP hydrolysis or both.Tariquidar can be considered an ideal agent for testing the role of P-glycoprotein inhibition in cancer

ChEBI: Tariquidar is a member of benzamides.

Specific inhibitor of MDR-1 (P-gp)

P-glycoprotein

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[2] EDNA F CHOO. Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier.[J]. Journal of Pharmacology and Experimental Therapeutics, 2006, 317 3: 1012-1018. DOI: 10.1124/jpet.105.099648