2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. Cytochrome P450 RAR/RXR
  4. Liarozole dihydrochloride

Liarozole dihydrochloride  (Synonyms: R75251 dihydrochloride)

Cat. No.: HY-106019C Purity: ≥99.0%
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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

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5 mg USD 150 In-stock
10 mg USD 240 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Liarozole dihydrochloride:

Liarozole dihydrochloride Related Antibodies

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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

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].

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

Liarozole dihydrochloride Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1.[H]Cl.[H]Cl
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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (261.99 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥99.0%

COA (253 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.6199 mL 13.0996 mL 26.1993 mL 65.4982 mL
5 mM 0.5240 mL 2.6199 mL 5.2399 mL 13.0996 mL
10 mM 0.2620 mL 1.3100 mL 2.6199 mL 6.5498 mL
15 mM 0.1747 mL 0.8733 mL 1.7466 mL 4.3665 mL
20 mM 0.1310 mL 0.6550 mL 1.3100 mL 3.2749 mL
25 mM 0.1048 mL 0.5240 mL 1.0480 mL 2.6199 mL
30 mM 0.0873 mL 0.4367 mL 0.8733 mL 2.1833 mL
40 mM 0.0655 mL 0.3275 mL 0.6550 mL 1.6375 mL
50 mM 0.0524 mL 0.2620 mL 0.5240 mL 1.3100 mL
60 mM 0.0437 mL 0.2183 mL 0.4367 mL 1.0916 mL
80 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
100 mM 0.0262 mL 0.1310 mL 0.2620 mL 0.6550 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Liarozole dihydrochloride 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.

Keywords:

Liarozole1883548-96-6R75251R 75251R-75251Cytochrome P450RAR/RXRCYPsRetinoic acid receptorsRetinoid X receptorsSCIDOvariectomizedMCF-7MesenchymalImidazoleHydroxylationInhibitorinhibitorinhibit

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