Synonyms: (B)-N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine; (R)-N-[4-[2-Ethyl-1-(1H-1,2,4-triazol(-1-yl)butyl]phenyl]-2-benzothiazolamine; TLZ; Talarozole
Molecular Formula: C21H23N5S
Molecular Weight: 377.51
Linear Structural Formula: C21H23N5S
MDL Number: MFCD13194908
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: R115866 (Talarozole) is an orally active all-trans retinoic acid (RA) metabolism blocking agent (RAMBA; IC50 = 4 nM against RA metablism in yeast microsomes expressing human CYP26) with much reduced or little potency against CYP19 (aromatase), CYP17 (17,20-lyase), CYP2C11, CYP3A, and CYP2A1 (IC50 from 1.2 to >10 muM). Plasma and tissue RA upregulation via R115866 oral treatment exhibits in vivo efficacy in several retinoid-responsive rodent models, including vaginal keratinization suppression (ED50 = 1.0 mg/kg/day vs. 5.1 mg/kg/day with RA in rats), pinnal hyperplasia induction (ear epidermis thickness = 35.5 mum with 2.5 mg/kg/day R115866 vs. 16.5 mum in control mice), conversion of caudal para- to ortho-keratosis (90% with 1.25 mg/kg/day R115866 vs. 30.3% in control mice). Comparing to liarozole, R115866 is CYP26-selective and does not inhibit CYP-mediated biosynthesis of adrenal and gonadal steroid hormones.