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201410-53-9

中文名稱 他拉羅唑
英文名稱 R 115866
CAS 201410-53-9
分子式 C21H23N5S
分子量 377.51
MOL 文件 201410-53-9.mol
更新日期 2024/11/15 18:20:28
201410-53-9 結(jié)構(gòu)式 201410-53-9 結(jié)構(gòu)式

基本信息

中文別名
N-(4-(2-乙基-1-(1H-1,2,4-三唑-1-基)丁基)苯基)苯并[D]噻唑-2-胺
英文別名
R 115866
RaMbazole
RAMBAZOLE
R115866
R-115866
R 115866
N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine
N-(4-(2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl)phenyl)benzo[d]thiazol-2-amine)

物理化學(xué)性質(zhì)

沸點(diǎn)561.0±60.0 °C(Predicted)
密度1.26±0.1 g/cm3(Predicted)
儲(chǔ)存條件Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)2.70±0.10(Predicted)
形態(tài)粉末
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

常見問題列表

生物活性
Talarozole (R115866) 是一種口服性全反式維甲酸代謝阻斷劑 (RAMBA),可提高內(nèi)源性全反式維甲酸 (RA) 的細(xì)胞內(nèi)水平。Talarozole 抑制 CYP26A1 和 CYP26B1,IC50 值分別為 5.4 和 0.46 nM。
靶點(diǎn)

IC50: 0.46/5.1 nM (CYP26B1/A1)

體外研究

When HepG2 cells are cotreated with atRA and Talarozole (1 μM), 4-OH-RA and 4-oxo-RA formation is significantly decreased.

體內(nèi)研究

A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) C max of 80 nM and a K i of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, at RA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased at RA concentrations. In agreement, at RA concentrations are elevated in serum and liver at all timepoints measured. This increase in at RA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice.

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