R115866

产品名称：

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

产品介绍：

产品说明

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.

基本信息

经验(实验)分子式	C₂₁H₂₃N₅S
分子量	377.51
MDL编号	MFCD13194908
NACRES	NA.77

产品性质

测定	≥98% (HPLC)
形式	film
颜色	colorless
溶解性	DMSO: 2 mg/mL, clear
储存温度	2-8℃

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable