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R115866
产品别名
870093-23-5
R115866
(R)-N-[4-[2-Ethyl-1-(1H-1,2,4-triazol(-1-yl)butyl]phenyl]-2-benzothiazolamine
Talarozole
(B)-N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine
TLZ
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C21H23N5S |
| Molecular weight | 377.51 |
| MDL number | MFCD13194908 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | 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. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | film |
| color【颜色】 | colorless |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
