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SML2040 Sigma-Aldrich

Liarozole dihydrochloride

≥98% (HPLC)

Synonym: 5-[(3-Chlorophenyl)(1H-imidazol-1-yl)methyl]-1H-benzimidazole, 6-[(3-Chlorophenyl)(1H-imidazol-1-yl)methyl]-1H-benzimidazole dihydrochloride, R 75251 dihydrochloride, R-75251 dihydrochloride, R75251 dihydrochloride

  • CAS Number 1883548-96-6

  • Empirical Formula (Hill Notation) C17H13ClN4 · 2HCl

  • Molecular Weight 381.69

  •  NACRES NA.77

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, L
assay   ≥98% (HPLC)
form   powder
storage condition   desiccated
color   white to beige
solubility   H2O: 2 mg/mL, clear
storage temp.   room temp
SMILES string   ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1

Description

Biochem/physiol Actions

Liarozole (R 75251, R75,251) is an orally active benzimidazole-based retinoic acid (RA) metabolism blocking agent (RAMBA) that targets multiple P450 enzymes, including aromatase (CYP19), 17-hydroxylase/17,20-lyase (CYP17A1), 11-hydroxylase (CYP11B1), and RA 4-hydroxylase (CYP26). Liarozole is more effective than ketoconazole in vivo (plasma RA enhancement = 2.5 ng/mL vs. 1.3 ng/mL 2 hr after respective oral dosage of 40 mg/kg in rats) and, in contrast to ketoconazole, Liarozole does not significantly affect circulating adrenal androgen levels. Liarozole is shown to effectively suppress androgen-dependent tumor expansion of R3327G Dunning prostate adenocarcinoma xenografts in rats (by 66% and 81% with 80 and 120 mg/kg/day p.o., respectively) independent of its androgen biosynthesis inhibition.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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