406191-34-2
中文名稱
5-chloro-N'-[2-(trifluoromethyl)phenyl]sulfonyl-1-benzofuran-2-carbohydrazide
英文名稱
5-chloro-N'-[2-(trifluoromethyl)phenyl]sulfonyl-1-benzofuran-2-carbohydrazide
CAS
406191-34-2
分子式
C16H10ClF3N2O4S
分子量
418.77
MOL 文件
406191-34-2.mol
406191-34-2 結(jié)構(gòu)式
基本信息
中文別名
化合物BCATC INHIBITOR 2 英文別名
BCATc Inhibitor 25-chloro-N'-[2-(trifluoromethyl)phenyl]sulfonyl-1-benzofuran-2-carbohydrazide
2-Benzofurancarboxylic acid, 5-chloro-, 2-[[2-(trifluoromethyl)phenyl]sulfonyl]hydrazide
物理化學(xué)性質(zhì)
儲(chǔ)存條件Store at -20°C, protect from light
溶解度≤10mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
形態(tài)結(jié)晶固體
顏色White to off-white
常見問題列表
生物活性
BCATc Inhibitor 2 是一種選擇性的分支鏈氨基轉(zhuǎn)移酶 (BCAT) 抑制劑，可用于神經(jīng)退行性疾病的研究。對 rBCATc，hBCATc 和 rBCATm 的 IC50 分別為 0.2 μM，0.8 μM 和 3.0 μM。BCATc 也叫 BCAT1，存在于細(xì)胞質(zhì)基質(zhì)中的亞型。靶點(diǎn)
IC50: 0.2 μM (rBCATc), 0.8 μM (hBCATc), 3.0 μM (rBCATm).
體外研究
BCATc Inhibitor 2 decreases calcium influx in neuronal cultures with an IC 50 =4.8±1.2 μM.
體內(nèi)研究
BCATc Inhibitor 2 also blocks calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrates neuroprotective efficacy in vivo.
Following a 30 mg/kg subcutaneous injection to Lewis rats, BCATc Inhibitor 2 reaches a peak plasma concentration (Cmax) of 8.28 μg/mL at 0.5 h (t
max
). The mean plasma exposure (AUC) value is 19.9 μg h/mL, and the mean terminal half-life ranged from 12 to 15 h, indicating favorable PK parameters of BCATc Inhibitor 2.