Liarozole dihydrochloride 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.

Liarozole inhibits 17a-hydroxylase activity in bovine adrenal microsomes (IC50=0.15 μM) [1]. Liarozole has modest inhibitory activity on cholesterol synthesis in human hepatoma cells(IC50=5 μM)[1].Liarozole inhibits the metabolism of retinoic acid to more polar metabolites in hamster liver microsomes (IC50=2.2 μM), rat liver homogenate (IC50=0.14 μM), dunning prostate cancer homogenate (IC50=0.26 μM) and MCF-7 human breast cancer cells (almost complete block at 10μM) [1].

1883548-96-6

C17H15Cl3N4

381.69

R75251 dihydrochloride;Liarozole dihydrochloride

H2O:50 mg/mL (131.00 mM)
DMSO:50 mg/mL (131.00 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years