Tariquidar

- Overview
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    Background
    
    Tariquidar is a potent inhibitor of P-glycoprotein (Pgp), a 170-kDa transmembrane protein acting as a drug efflux pump to actively transport structurally unrelated compounds out of cells, that noncompetitively inhibits the basal the activity of ATPase associated with Pgp. Tariquidar contains a tertiary amine, dimethoxyphenyl group and amide group in its chemical structure, which contribute to its inhibition against Pgp. Results of in vitro assays of three different models have shown that Tariquidar inhibits Pgp with 50% inhibition concentration IC50 values ranging from 15 to 223 nM. However, the inhibition by tariquidar is Pgp-specific and attenuated in tumor cell lines, where multidrug resistance is mediated by multidrug resistance-associated protein.
- Properties
  - Alternative Name
    
    XR9576, XR 9576, XR-9576,Tariquidar; N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide
    
    CAS Number
    
    206873-63-4
    
    Molecular Formula
    
    C38H38N4O6
    
    Molecular Weight
    
    646.73
    
    Appearance
    
    A solid
    
    Purity
    
    98.79%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥16.17 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Aleksandra Filipiak-Duliban, Klaudia Brodaczewska, et al. "Spheroid Culture Differentially Affects Cancer Cell Sensitivity to Drugs in Melanoma and RCC Models." Int J Mol Sci. 2022 Jan 21;23(3):1166. PMID:35163092
    2. Natalia Kasica, Piotr Jakubowski, et al. "P-Glycoprotein Inhibitor Tariquidar Plays an Important Regulatory Role in Pigmentation in Larval Zebrafish." Cells. 2021 Mar 20;10(3):690. PMID:33804686
    3. Mohammadpour R, Safarian S, et al. "Comparative Endocytosis Mechanisms and Anticancer Effect of HPMA Copolymer- and PAMAM Dendrimer-MTCP Conjugates for Photodynamic Therapy." Macromol Biosci. 2016 Oct 25. PMID:27779358
    4. Sajja, Ravi K., and Luca Cucullo. "Altered glycaemia differentially modulates efflux transporter expression and activity in hCMEC/D3 cell line." Neuroscience letters 598 (2015): 59-65. PMID:25982326

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Tariquidar

Background

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