Tariquidar
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
- 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.
Definition
ChEBI: Tariquidar is a member of benzamides.
Biochem/physiol Actions
Specific inhibitor of MDR-1 (P-gp)
target
P-glycoprotein
TariquidarSupplier
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Tariquidar(206873-63-4)Related Product Information
- Diphenyldiethoxysilane
- XR9576
- AC480 (BMS-599626)
- ISOXADIFEN-ETHYL
- PHENYL VALERATE
- p-(2-Methoxyethyl) phenol
- Diphenyldimethoxysilane
- Ethyl acetate
- Ethyl acrylate
- Ethyl formate
- Ethanol
- Ethylparaben
- 4-Methoxyphenylacetone
- Isoquinoline
- Methoxydiethylborane
- PHENYL RESIN
- 4-[2-(3,4-DIHYDRO-6,7-DIMETHOXY-2(1H)-ISOQUINOLINYL)ETHYL]-BENZENAMINE
- Tariquidar