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

Liarozole dihydrochloride (Synonyms: R75251 dihydrochloride)

Cat. No.: HY-106019C Purity: ≥99.0%
Handling Instructions

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

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

Liarozole dihydrochloride Chemical Structure

Liarozole dihydrochloride Chemical Structure

CAS No. : 1883548-96-6

Size Price Stock Quantity
1 mg USD 95 In-stock
Estimated Time of Arrival: December 31
5 mg   Get quote  
10 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Liarozole dihydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

Cytochrome P450 (CYP26)

7 μM (IC50)

In Vitro

Liarozole dihydrochloride (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation[3].
Liarozole dihydrochloride (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 dihydrochloride (5-20 mg/kg; p.o.) reverses the vaginal keratosis caused by estrogen stimulation[5].
Liarozole dihydrochloride (40 mg/kg; p.o.) 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.
Result: Reversed the vaginal keratosis caused by estrogen stimulation.
Animal Model: SCID mice
Dosage: 40 mg/kg
Administration: P.o.
Result: Inhibited tumor growth and survival.
Clinical Trial
Molecular Weight

381.69

Formula

C₁₇H₁₅Cl₃N₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (131.00 mM)

DMSO : 50 mg/mL (131.00 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6199 mL 13.0996 mL 26.1993 mL
5 mM 0.5240 mL 2.6199 mL 5.2399 mL
10 mM 0.2620 mL 1.3100 mL 2.6199 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: ≥ 2.08 mg/mL (5.45 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

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

Purity: ≥99.0%

  • 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 dihydrochloride
Cat. No.:
HY-106019C
Quantity:
MCE Japan Authorized Agent: