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| Tariquidar Basic information |
| Product Name: | Tariquidar | | Synonyms: | N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxy-phenyl]quinoline-3-carboxamide;Tariquidar;3-Quinolinecarboxamide, N-(2-(((4-(2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl)phenyl)amino)carbonyl)-4,5-dimethoxyphenyl)-;N-(2-((4-(2-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)carbamoyl)-4,5-dimethoxyphenyl)quinoline-3-carboxamide;Unii-J58862dtvd;Xr 9576;Xr9576;N-[2-[N-[4-[2-(6,7-DiMethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl]carbaMoyl]-4,5-diMethoxyphenyl]quinoline-3-carboxaMide | | CAS: | 206873-63-4 | | MF: | C38H38N4O6 | | MW: | 646.73 | | EINECS: | | Product Categories: | Inhibitors;Anti-cancer&immunity;Inhibitor | | Mol File: | 206873-63-4.mol |
| Tariquidar Chemical Properties |
| Melting point | >190oC (dec.) | | Boiling point | 716.0±60.0 °C(Predicted) | | density | 1.276±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | powder | | pka | 10.67±0.70(Predicted) | | color | white to light brown |
| Tariquidar Usage And Synthesis |
| Description | Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (Kd = 5.1 nM) and inhibits transport activity. It inhibits transport of vinblastine and paclitaxel in multidrug resistant CHrB30 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. | | Uses | 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 | | Uses | 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. | | Biochem/physiol Actions | Specific inhibitor of MDR-1 (P-gp) |
| Tariquidar Preparation Products And Raw materials |
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