Art. -Nr.: HY-106019

Liarozole

(Synonyms: R75251)

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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.

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Reinheit: 98.96%
CAS. Nr.: 115575-11-6
Formel: C₁₇H₁₃ClN₄
Molecular Weight:308.76

Speicherung:

4°C, protect from light

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

Liarozole Chemical Structure

CAS. Nr.: 115575-11-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CYP26

7 μM (IC₅₀)

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Alle RAR/RXR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.89 μM Compound: Liarozole	Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins in dark condition with NADPH and ATRA by HPLC method Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins in dark condition with NADPH and ATRA by HPLC method	[PMID: 26365710]
HL-60	IC₅₀	2.45 μM Compound: Liarozole	Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins using ATRA and NADPH by HPLC method Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins using ATRA and NADPH by HPLC method	[PMID: 25684424]
MCF7	IC₅₀	540 nM Compound: Liarozole	Inhibition of CYP26A1 in human MCF7 cell microsomes using [3H]ATRA after 1 hr by scintillation counting Inhibition of CYP26A1 in human MCF7 cell microsomes using [3H]ATRA after 1 hr by scintillation counting	[PMID: 21428449]
MCF7	IC₅₀	7 μM Compound: liarozole	Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism	[PMID: 16279770]
MCF7	IC₅₀	7 μM Compound: Liarozole	Inhibition of CYP26A1 in human MCF7 cells Inhibition of CYP26A1 in human MCF7 cells	[PMID: 18722776]
Sf9	IC₅₀	0.018 μM Compound: 1	Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]
Sf9	IC₅₀	1.9 μM Compound: 1	Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]
SH-SY5Y	IC₅₀	2.3 nM Compound: Liar	Increase in CYP26A1 mRNA expression in human SH-SY5Y cells after 72 hrs by RT-PCR analysis in the presence of 0.1 uM all-trans-retinoic acid Increase in CYP26A1 mRNA expression in human SH-SY5Y cells after 72 hrs by RT-PCR analysis in the presence of 0.1 uM all-trans-retinoic acid	[PMID: 21838328]

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].

MedChemExpress (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].

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

Animal Model:

Ovariectomized rats^[5]
Dosage:

5~20 mg/kg
Administration:

P.o.; 3 days
Result:

Reversed the vaginal keratosis caused by estrogen stimulation.

Animal Model:

SCID mice^[6]
Dosage:

40 mg/kg
Administration:

P.o.; 21 days
Result:

Inhibited tumor growth and survival.

Chemical Information

CAS. Nr. 115575-11-6
Appearance Solid
Molecular Weight 308.76
Formel C₁₇H₁₃ClN₄
Color Off-white to light yellow
SMILES

ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1
Synonyms

R75251
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (323.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kuijpers AL, et al. The effects of oral liarozole on epidermal proliferation and differentiation in severe plaque psoriasis are comparable with those of acitretin. Br J Dermatol. 1998;139(3):380-389. [Content Brief]

[2]. Lucker GP, et al. Oral treatment of ichthyosis by the cytochrome P-450 inhibitor liarozole. Br J Dermatol. 1997;136(1):71-75. [Content Brief]

[3]. Wouters W, et al. Effects of liarozole, a new antitumoral compound, on retinoic acid-induced inhibition of cell growth and on retinoic acid metabolism in MCF-7 human breast cancer cells. Cancer Res. 1992;52(10):2841-2846. [Content Brief]

[4]. Pignatello MA, et al. Liarozole markedly increases all trans-retinoic acid toxicity in mouse limb bud cell cultures: a model to explain the potency of the aromatic retinoid (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl] benzo [Content Brief]

[5]. Van Wauwe J, et al. Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J Pharmacol Exp Ther. 1992;261(2):773-779. [Content Brief]

[6]. Stearns ME, et al. Liarozole and 13-cis-retinoic acid anti-prostatic tumor activity [published correction appears in Cancer Res 1993 Dec 1;53(23):5831]. Cancer Res. 1993;53(13):3073-3077. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2388 mL	16.1938 mL	32.3876 mL	80.9690 mL
	5 mM	0.6478 mL	3.2388 mL	6.4775 mL	16.1938 mL
	10 mM	0.3239 mL	1.6194 mL	3.2388 mL	8.0969 mL
	15 mM	0.2159 mL	1.0796 mL	2.1592 mL	5.3979 mL
	20 mM	0.1619 mL	0.8097 mL	1.6194 mL	4.0485 mL
	25 mM	0.1296 mL	0.6478 mL	1.2955 mL	3.2388 mL
	30 mM	0.1080 mL	0.5398 mL	1.0796 mL	2.6990 mL
	40 mM	0.0810 mL	0.4048 mL	0.8097 mL	2.0242 mL
	50 mM	0.0648 mL	0.3239 mL	0.6478 mL	1.6194 mL
	60 mM	0.0540 mL	0.2699 mL	0.5398 mL	1.3495 mL
	80 mM	0.0405 mL	0.2024 mL	0.4048 mL	1.0121 mL
	100 mM	0.0324 mL	0.1619 mL	0.3239 mL	0.8097 mL

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Liarozole

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High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Liarozole

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Rare Diseases Drug Library

Protein-protein Interaction Inhibitor Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Nuclear Receptor Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Liarozole Related Classifications

HY-106019 Related Classifications