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

Liarozole dihydrochloride (Synonyms: R75251 dihydrochloride)

Cat. No.: HY-106019C
Handling Instructions

Liarozole dihydrochloride (R75251; R85246) 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 prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. 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.

For research use only. We do not sell to patients.

Liarozole dihydrochloride Chemical Structure

Liarozole dihydrochloride Chemical Structure

CAS No. : 1883548-96-6

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Description

Liarozole dihydrochloride (R75251; R85246) 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 prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. 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[1].

In Vitro

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].
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].

Molecular Weight

381.69

Formula

C₁₇H₁₅Cl₃N₄

CAS No.

1883548-96-6

SMILES

ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1.[H]Cl.[H]Cl

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (131.00 mM)

DMSO : 50 mg/mL (131.00 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

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Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6199 mL 13.0996 mL 26.1993 mL
5 mM 0.5240 mL 2.6199 mL 5.2399 mL
10 mM 0.2620 mL 1.3100 mL 2.6199 mL
*Please refer to the solubility information to select the appropriate solvent.
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Liarozole dihydrochloride
Cat. No.:
HY-106019C
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