| Identification | Back Directory | [Name]
Talarozole | [CAS]
870093-23-5 | [Synonyms]
talarozole
(R)-Talarozole
Talarozole (R enantiomer)
N-[4-[(1R)-2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine
2-Benzothiazolamine, N-[4-[(1R)-2-ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]- | [Molecular Formula]
C21H23N5S | [MDL Number]
MFCD13194908 | [MOL File]
870093-23-5.mol | [Molecular Weight]
377.51 |
| Chemical Properties | Back Directory | [Boiling point ]
561.0±60.0 °C(Predicted) | [density ]
1.26 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: ≥ 51 mg/mL (135.10 mM) | [form ]
film | [pka]
2.70±0.10(Predicted) | [color ]
colorless |
| Hazard Information | Back Directory | [Uses]
Talarozole is a retinoic acid metabolism blocking agent (RAMBA) that can be used for treating dermatalogical diseases such as psoriasis and acne. | [Definition]
ChEBI: An N-{4-[2-ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl}-1,3-benzothiazol-2-amine that is the (R)-enantiomer of talarozole. The racemate is used for the treatment of keratinization disorders, psoriasis
nd acne. | [Biological Activity]
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)CYP2C11CYP3Aand CYP2A1 (IC50 from 1.2 to >10 μM). Plasma and tissue RA upregulation via R115866 oral treatment exhibits in vivo efficacy in several retinoid-responsive rodent modelsincluding 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 μm with 2.5 mg/kg/day R115866 vs. 16.5 μm 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 liarozoleR115866 is CYP26-selective and does not inhibit CYP-mediated biosynthesis of adrenal and gonadal steroid hormones. |
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