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

Zosuquidar (Synonyms: LY335979)

Cat. No.: HY-15255 Purity: 98.33%
Handling Instructions

Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.

For research use only. We do not sell to patients.

Zosuquidar Chemical Structure

Zosuquidar Chemical Structure

CAS No. : 167354-41-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 864 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Zosuquidar:

Top Publications Citing Use of Products

    Zosuquidar 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

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    Description

    Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. IC50 value: 60 nM (Ki) Target: P-glycoprotein Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM. Zosuquidar binds with high affinity to P-glycoprotein and inhibits P-glycoprotein-mediated multidrug resistance (MDR). P-glycoprotein, encoded by the MDR-1 gene, is a member of the ATP-binding cassette superfamily of transmembrane transporters and prevents the intracellular accumulation of many natural product-derived cytotoxic agents. Zosuquidar is a compound of antineoplastic drug candidates currently under development.

    Clinical Trial
    Molecular Weight

    527.60

    Formula

    C₃₂H₃₁F₂N₃O₂

    CAS No.

    167354-41-8

    SMILES

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 8.33 mg/mL (15.79 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8954 mL 9.4769 mL 18.9538 mL
    5 mM 0.3791 mL 1.8954 mL 3.7908 mL
    10 mM 0.1895 mL 0.9477 mL 1.8954 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.83 mg/mL (1.57 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 0.83 mg/mL (1.57 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.83 mg/mL (1.57 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    ZosuquidarLY335979LY 335979LY-335979P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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    Product name:
    Zosuquidar
    Cat. No.:
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