双醋酚丁

中文名称:

双醋酚丁

中文同义词:

双醋酚丁;双醋酚丁 标准品;双醋酚丁衍生物;双丙酚丁;双丙富马酸盐

英文名称:

oxyphenisatine di(acetate)

英文同义词:

oxyphenisatine di(acetate);OXYPHENISATIN ACETATE;Isapheninum;Isaphenin;3,3-Bis[4-(acetyloxy)phenyl]-1,3-dihydro-2H-indol-2-one;Isocrin;Levema;NSC-59687

CAS号:

115-33-3

分子式:

C24H19NO5

分子量:

401.41

EINECS号:

204-083-6

相关类别:

通便;医药原料;对照品

Mol文件:

115-33-3.mol

熔点 

244℃

沸点 

566.5±50.0 °C(Predicted)

密度 

1.282±0.06 g/cm3(Predicted)

酸度系数(pKa)

13.55±0.40(Predicted)

用途

双醋酚丁是一种化学物质，临床药品口服后在肠内遇碱性肠液逐渐分解成醋酸和酚丁，酚丁对肠粘膜的刺激作用比酚肽强数十倍，故其导泻作用较强。

生物活性

Oxyphenisatin acetate是oxyphenisatin的前体药物，过去常用作泻药。

体外研究

Oxyphenisatin acetate inhibits the growth of the breast cancer cell lines MCF7, T47D, HS578T, and MDA-MB-468. In the estrogen receptor (ER) positive MCF7 and T47D cells, oxyphenisatin acetate induces TNFα expression and TNFR1 degradation, indicating autocrine receptor-mediated apoptosis in these lines. Ten micromoles per liter Oxyphenisatin acetate treatment results in autophagy and mitochondrial dysfunction.

体内研究

Oxyphenisatin acetate (300 mg/kg, i.p.) delivers intraperitoneally inhibited tumor growth, accompanied by phosphorylation of eIF2α and degradation of TNFR1 in an MCF7 xenograft model.

毒性

LD50 oral in rat: 1900mg/kg