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 (K_d = 5.1 nM) and inhibits transport activity. It inhibits transport of vinblastine and paclitaxel 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.

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.

Definition

ChEBI: Tariquidar is a member of benzamides.

Biochem/physiol Actions

Specific inhibitor of MDR-1 (P-gp)

target

P-glycoprotein

Tariquidar(206873-63-4)Related Product Information

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