Tariquidar dihydrochloride

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Cat.No. 5757 - Tariquidar dihydrochloride | C38H38N4O6.2HCl
Description: Potent P-glycoprotein (P-gp) inhibitor
Chemical Name: N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarbxamide dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent P-glycoprotein (P-gp) inhibitor (IC50 = 5.1 nM). Reverses drug resistance in multiple MDR cell lines. Acts as a substrate for breast cancer resistance protein (BCRP) at low concentrations and acts as an inhibitor of BCRP when used at >100 nM concentration. Potentiates the cytotoxic effects of doxorubicin (Cat. No. 2252) and mitoxantrone (Cat. No. 4250) in vitro.

Technical Data

M. Wt 719.66
Formula C38H38N4O6.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 121513890
InChI Key ZJCJRGRTDKIFJJ-UHFFFAOYSA-N
Smiles O=C(C1=CC(OC)=C(OC)C=C1NC(C2=CN=C(C=CC=C3)C3=C2)=O)NC(C=C4)=CC=C4CCN5CC6=CC(OC)=C(OC)C=C6CC5.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 71.97 100

Preparing Stock Solutions

The following data is based on the product molecular weight 719.66. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.39 mL 6.95 mL 13.9 mL
5 mM 0.28 mL 1.39 mL 2.78 mL
10 mM 0.14 mL 0.69 mL 1.39 mL
50 mM 0.03 mL 0.14 mL 0.28 mL

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References

References are publications that support the biological activity of the product.

Kannan et al (2011) The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2). ACS Chem.Neurosci. 2 82 PMID: 22778859

Loo et al (2015) Mapping the binding site of the inhibitor Tariquidar that stabilizes the first transmembrane domain of P-glycoprotein. J.Biol.Chem. 290 29389 PMID: 26507655


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Citations for Tariquidar dihydrochloride

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