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Liarozole (R75251 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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $76 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $328 | In Stock | |
25 mg | $558 | In Stock | |
50 mg | $788 | In Stock | |
100 mg | $1,120 | In Stock | |
1 mL x 10 mM (in DMSO) | $226 | In Stock |
Description | Liarozole (R75251 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. |
Targets&IC50 | CYP26:7 μM (IC50) |
In vitro | 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]. |
Alias | R75251 dihydrochloride |
Molecular Weight | 308.76 |
Formula | C17H13ClN4 |
Cas No. | 115575-11-6 |
Smiles | Clc1cccc(c1)C(c1ccc2nc[nH]c2c1)n1ccnc1 |
Relative Density. | 1.36g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (178.13 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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