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Tariquidar

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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
Product Categories:
  • Inhibitors
  • Anti-cancer&immunity
  • Inhibitor
Mol File:
206873-63-4.mol
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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
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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

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