Liarozole

Research use only, not for human use.

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 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.

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.

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 miceDosage:40 mg/kg Administration:P.o.; 21 days Result:Inhibited tumor growth and survival.

R75251 dihydrochloride

Metabolic Enzyme/Protease

P450

CYP450

——

——

115575-11-6

308.76

C17H13ClN4

>98% (HPLC)

DMSO:10 mM

ClC1=CC(C(C2=CC=C3NC=NC3=C2)N4C=CN=C4)=CC=C1

——

(-20℃)

With Ice Pack

≥ 2 years