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

Itraconazole  (Synonyms: R51211)

Cat. No.: HY-17514 Purity: 99.81%
COA 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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Based on 15 publication(s) in Google Scholar

Other Forms of Itraconazole:

Itraconazole Related Antibodies

Top Publications Citing Use of Products

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

    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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    Itraconazole Related Antibodies
    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].

    MedChemExpress (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

    Appearance

    Solid

    Formula

    C35H38Cl2N8O4
    CAS No.
    SMILES

    ClC1=C(C=CC(Cl)=C1)[C@@]2(O[C@@H](COC3=CC=C(N4CCN(C5=CC=C(N(C=NN6C(C)CC)C6=O)C=C5)CC4)C=C3)CO2)CN7C=NC=N7
    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 available by MedChemExpress (MCE).
    Purity & Documentation
    References
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    Itraconazole Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Itraconazole84625-61-6R51211R 51211R-51211FungalHedgehogCytochrome P450AutophagyAntibioticBacterialCYPsTriazoleantifungalHhanticancerCYP-450antiangiogenic14α-demethylaselanosterolergosterolInhibitorinhibitorinhibit

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