Liarozole

SKU: orb1219076

Description

Liarozole is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders. (In Vitro):Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation.Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis.(In Vivo):Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation.Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially.

Key Properties

• CAS Number: 115575-11-6
• MW: 308.76
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₃ClN₄
• SMILES: ClC1=CC(C(C2=CC=C3NC=NC3=C2)N4C=CN=C4)=CC=C1
• Target: P450
• Solubility: DMSO:10 mM

Bioactivity

• In Vivo:
  Liarozole (5-20 mg/kg; p.o. ; 3 days) reverses the vaginal keratosis caused by estrogen stimulation. Liarozole (40 mg/kg; p.o. ; 21 days) reduces tumor burden substantially. 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.
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• In Vitro:
  Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation. Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis. Cell Proliferation Assay 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 Cell line: Mesenchymal cells. Concentration: 1 μM. Incubation time: 4 days. Result: Completely inhibited chondrogenesis.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

R75251 dihydrochloride

Quick Database Links

Gene Symbol

P450