SML2092
R115866
≥98% (HPLC), RAMBA blocker, film
别名:
(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
登录 查看组织和合同定价。
选择规格
变更视图
关于此项目
经验公式（希尔记法）:
C21H23N5S
化学文摘社编号:
分子量:
377.51
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
film
产品名称
R115866, ≥98% (HPLC)
assay
≥98% (HPLC)
form
film
color
colorless
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
[s]1c2c(nc1Nc3ccc(cc3)[C@H]([n]4ncnc4)C(CC)CC)cccc2
InChI
1S/C21H23N5S/c1-3-15(4-2)20(26-14-22-13-23-26)16-9-11-17(12-10-16)24-21-25-18-7-5-6-8-19(18)27-21/h5-15,20H,3-4H2,1-2H3,(H,24,25)/t20-/m1/s1
InChI key
SNFYYXUGUBUECJ-HXUWFJFHSA-N
Biochem/physiol Actions
Orally active retinoic acid (RA) metabolism blocking agent (RAMBA) with higher CYP26 specificity and potency than liarozole (R75251).
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable