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

Liarozole (Synonyms: R75251)

Cat. No.: HY-106019
Handling Instructions

Liarozole (R75251; R85246) is an imidazole derivative and a 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

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10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Liarozole (R75251; R85246) is an imidazole derivative and a 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.; once daily for 3 days) reverses the vaginal keratosis caused by estrogen stimulation[5].
Liarozole (40 mg/kg; guvage; 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.
Molecular Weight

308.76

Formula

C₁₇H₁₃ClN₄

CAS No.
SMILES

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

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)

References
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Keywords:

LiarozoleR75251R 75251R-75251Cytochrome P450CYPsSCIDOvariectomizedMCF-7MesenchymalImidazoleHydroxylationInhibitorinhibitorinhibit

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