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Liarozole is an inhibitor of the cytochrome P450 (CYP) isoform CYP26A1 (IC50 = 2.1 µM), an enzyme involved in the metabolism of all-trans retinoic acid (Cay-11017). It also inhibits the production of estradiol (Cay-10006315) induced by follicle-stimulating hormone (FSH) in rat granulosa cells and testosterone and androstenedione production induced by human chorionic gonadotropin (hCG) in rat testicular cells (IC50s = 0.4, 2.3, and 0.7 µM, respectively). Liarozole enhances the antiproliferative activity of all-trans retinoic acid in MCF-7 breast cancer cells. It decreases plasma levels of retinoic acid in rats in a dose-dependent manner. Liarozole (5 and 20 mg/kg) decreases estradiol undecylate-induced vaginal keratinization in ovariectomized rats.Formal Name: 6-[(3-chlorophenyl)-1H-imidazol-1-ylmethyl]-1H-benzimidazole. CAS Number: 115575-11-6. Synonyms: R 75251. Molecular Formula: C17H13ClN4. Formula Weight: 308.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: ClC1=CC=CC(C(N2C=NC=C2)C3=CC=C(N=CN4)C4=C3)=C1. InChi Code: InChI=1S/C17H13ClN4/c18-14-3-1-2-12(8-14)17(22-7-6-19-11-22)13-4-5-15-16(9-13)21-10-20-15/h1-11,17H,(H,20,21). InChi Key: UGFHIPBXIWJXNA-UHFFFAOYSA-N.
Keywords:
R 75251, 6-[(3-chlorophenyl)-1H-imidazol-1-ylmethyl]-1H-benzimidazole
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