1. Metabolic Enzyme/Protease
  2. Cytochrome P450
    RAR/RXR
  3. Liarozole

Liarozole (Synonyms: R75251)

Cat. No.: HY-106019 Purity: 98.52%
Handling Instructions

Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.

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

Liarozole Chemical Structure

Liarozole Chemical Structure

CAS No. : 115575-11-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 275 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Liarozole:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].

IC50 & Target[1]

Cytochrome P450 (CYP26)

7 μM (IC50)

In Vitro

Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation[3].
Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis[4].

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

Cell Proliferation Assay[3]

Cell Line: MCF-7 cells
Concentration: 0.01~10 μM
Incubation Time: 9 days
Result: Had an effect of 35% inhibition at 10 μM on cell proliferation.

Cell Differentiation Assay[4]

Cell Line: Mesenchymal cells
Concentration: 1 μM
Incubation Time: 4 days
Result: Completely inhibited chondrogenesis.
In Vivo

Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation[5].
Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially[6].

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

Animal Model: Ovariectomized rats
Dosage: 5~20 mg/kg
Administration: P.o.; 3 days
Result: Reversed the vaginal keratosis caused by estrogen stimulation.
Animal Model: SCID mice
Dosage: 40 mg/kg
Administration: P.o.; 21 days
Result: Inhibited tumor growth and survival.
Clinical Trial
Molecular Weight

308.76

Formula

C₁₇H₁₃ClN₄

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 : 100 mg/mL (323.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2388 mL 16.1938 mL 32.3876 mL
5 mM 0.6478 mL 3.2388 mL 6.4775 mL
10 mM 0.3239 mL 1.6194 mL 3.2388 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: ≥ 2.5 mg/mL (8.10 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Liarozole
Cat. No.:
HY-106019
Quantity:
MCE Japan Authorized Agent: