1. Anti-infection
    Stem Cell/Wnt
    Metabolic Enzyme/Protease
    Autophagy
  2. Fungal
    Hedgehog
    Cytochrome P450
    Autophagy
    Antibiotic
  3. Itraconazole

Itraconazole (Synonyms: R51211)

Cat. No.: HY-17514 Purity: 99.15%
Handling Instructions

Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.

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

Itraconazole Chemical Structure

Itraconazole Chemical Structure

CAS No. : 84625-61-6

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Itraconazole:

Top Publications Citing Use of Products

    Itraconazole purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Sep 13;38(1):404.

    SCP2-OE GH3 cells are incubated with 10 μM itraconazole (ITR) for 48 h. The distribution of cholesterol (blue) in the different groups (Vector, SCP2-OE and SCP2-OE + ITR) are examined by filipin staining and laser confocal microscopy. Green signal, GH staining; red signal, PI nuclear staining. Scale bar, 10 μm.
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    Description

    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[1][2][3][4].

    IC50 & Target

    Fungal[1]
    IC50: ~800 nM (Hedgehog signaling pathway)[1]
    14α-demethylase (cytochrome P450 enzyme)[3]

    In Vitro

    Itraconazole has anti-proliferation of HUVEC (IC50 of 0.16 μM)[2].
    Itraconazole inhibits endothelial cell cycle progression at the G1 phase in vitro[1].

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

    In Vivo

    Itraconazole (75-100 mg/kg; oral gavage; twice per day; for 18 days; female outbred athymic nude mice) treatment suppresses Hh pathway activity and the growth of medulloblastoma in a mouse allograft model[1].

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

    Animal Model: Female outbred athymic nude mice (6-7-week-old) injected with Ptch+/− cells[1]
    Dosage: 75 mg/kg, 100 mg/kg
    Administration: Oral gavage; twice per day; for 18 days
    Result: Suppressed Hh pathway activity and the growth of medulloblastoma in a mouse allograft model.
    Clinical Trial
    Molecular Weight

    705.63

    Formula

    C₃₅H₃₈Cl₂N₈O₄

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 6.25 mg/mL (8.86 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4172 mL 7.0859 mL 14.1717 mL
    5 mM 0.2834 mL 1.4172 mL 2.8343 mL
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (28.34 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

    • 3.

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

      Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Product Name:
    Itraconazole
    Cat. No.:
    HY-17514
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