Talarozole
- Product Name
- Talarozole
- CAS No.
- 870093-23-5
- Chemical Name
- Talarozole
- 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]-
- CBNumber
- CB51518534
- Molecular Formula
- C21H23N5S
- Formula Weight
- 377.51
- MOL File
- 870093-23-5.mol
Talarozole Property
- 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)
- pka
- 2.70±0.10(Predicted)
- form
- film
- color
- colorless
N-Bromosuccinimide Price
- Product number
- API0013733
- Product name
- (R)-TALAROZOLE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $505.22
- Updated
- 2021/12/16
Talarozole Chemical Properties,Usage,Production
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), CYP2C11, CYP3A, and 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 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 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 liarozole, R115866 is CYP26-selective and does not inhibit CYP-mediated biosynthesis of adrenal and gonadal steroid hormones.
Talarozole Preparation Products And Raw materials
Raw materials
Preparation Products
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