Tariquidar
Synonym(s):N-[2-[[[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarboxamide;XR 9576;XR9576
- CAS NO.:206873-63-4
- Empirical Formula: C38H38N4O6
- Molecular Weight: 646.73
- MDL number: MFCD09837824
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-05 19:05:58
What is Tariquidar?
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.
The Uses of Tariquidar
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
The Uses of Tariquidar
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)
Properties of Tariquidar
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 |
Safety information for Tariquidar
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for Tariquidar
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