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%
Data Sheet SDS 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 $94 In-stock
10 mg $85 In-stock
50 mg $350 In-stock
100 mg $550 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

    Description

    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
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    References
    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
    [2]

    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
    [3][4]

    Rat: 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].

    Mouse: 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.

    References

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    Product Name:
    Zosuquidar trihydrochloride
    Cat. No.:
    HY-50671
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