1. Membrane Transporter/Ion Channel
  2. P-glycoprotein

Zosuquidar trihydrochloride (Synonyms: RS 33295-198 trihydrochloride; LY-335979 trihydrochloride)

Cat. No.: HY-50671 Purity: 98.75%
Handling Instructions

Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.

For research use only. We do not sell to patients.
Zosuquidar trihydrochloride Chemical Structure

Zosuquidar trihydrochloride Chemical Structure

CAS No. : 167465-36-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 112 In-stock
10 mg USD 102 In-stock
50 mg USD 420 In-stock
100 mg USD 660 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Zosuquidar trihydrochloride:

    Zosuquidar trihydrochloride purchased from MCE. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9.

    Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.

    IC50 & Target

    Ki: 59nM (P-glycoprotein)[1].

    In Vitro

    Zosuquidar completely or partially restores drug sensitivity in all P-gp-expressing leukemia cell lines and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AmL blasts with active P-gp. In addition, P-gp inhibition by zosuquidar is found to be more potent than cyclosporine A in cells with highly active P-gp[2].

    In Vivo

    Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain. An oral dose of 25 mg/kg of zosuquidar trihydrochloride increases the brain concentrations by about 2.5-fold at 1 h and 5-fold at 24 h after paclitaxel administrationbarrier[3]. Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner. Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6 h after a 2 mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20 mg/kg zosuquidar[4].

    Clinical Trial
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.5699 mL 7.8494 mL 15.6988 mL
    5 mM 0.3140 mL 1.5699 mL 3.1398 mL
    10 mM 0.1570 mL 0.7849 mL 1.5699 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay

    Cells are cultured in 96-well plates. Each drug of interest is added at escalating concentrations in the presence or absence of either zosuquidar or CsA. After 48 hour incubation (except Mylotarg, 4 days incubation), 20 μL of MTT is added to each well for a further 4 hour incubation. The purple precipitate is dissolved in 200 μL DMSO, and the optic density (OD) is determined by the multi-well plate reader[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Rats: Female Sprague-Dawley rats are used in the study. Zosuquidar solutions are prepared in 5% mannitol and adjusted to pH ~2.0 with concentrated HCl. Nelfinavir is infused (10 mg/kg/h) for up to 10 h with or without concurrent administration of an intravenous bolus dose of 2, 6, or 20 mg/kg zosuquidar given at 4 h. Brain tissue and plasma are analyzed for both drug concentrations[4].

    Mice: A stock solution of 5 mg/mL of zosuquidar trihydrochloride is prepared in vehicle solution and diluted in sterile saline. The vehicle solution consisted of 20 g/l mannitol and 1.5 g/l of glycine in water for injection and adjusted to a pH of 2.7 with hydrochloric acid. P-gp knockout mice and wild type mice are used as a model for complete inhibition of P-gp. Zosuquidar trihydrochloride is administered orally at 25 and 80 mg/kg 1 h before i.v. paclitaxel and i.v. at 20 mg/kg 10 min and 1 h before paclitaxel. The concentrations of paclitaxel in plasma and tissues and of zosuquidar trihydrochloride in plasma are quantified by high-performance liquid chromatography[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.



    FC1([[email protected]]2[[email protected]@H]1C3=C([[email protected]@H](C4=CC=CC=C42)N5CCN(CC5)C[[email protected]](COC6=C7C=CC=NC7=CC=C6)O)C=CC=C3)F.Cl.Cl.Cl

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Zosuquidar is dissolved in 20% ethanol-saline[5].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


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