格拉非宁 盐酸盐 CAS#: 65513-72-6

微信扫码

格拉非宁 盐酸盐

生物活性靶点体外研究体内研究

中文名称	格拉非宁 盐酸盐
中文同义词	格拉非宁 盐酸盐;2,3-二羟基丙基2-((7-氯喹啉-4-基)氨基)苯甲酸酯盐酸盐;盐酸格拉芬宁
英文名称	1-GLYCERYL N-[7-CHLORO-4-QUINOLYL]ANTHRANILATE HYDROCHLORIDE
英文同义词	GlafenineHCl;Glafenin hydrochloride;GLAFENINE HYDROCHLORIDE;1-GLYCERYL N-[7-CHLORO-4-QUINOLYL]ANTHRANILATE HYDROCHLORIDE;2,3-Dihydroxypropyl 2-((7-chloroquinolin-4-yl)amino)benzoate hydrochloride;inhibit,Glafenine Hydrochloride,Glafenine,Glafenin,Inhibitor
CAS号	65513-72-6
分子式	C19H18Cl2N2O4
分子量	409.26
EINECS号
相关类别	小分子抑制剂
Mol文件	65513-72-6.mol
结构式

格拉非宁 盐酸盐 性质

格拉非宁 盐酸盐 用途与合成方法

生物活性

Glafenine hydrochloride 是一种非甾体抗炎药 (NSAID), 具有镇痛活性。

靶点

IC50: 3.2 μM (ABCG2)

体外研究

Glafenine increases the surface expressionof mutant CFTR in baby hamster kidney (BHK) cells to 40% of that observed for wild-type CFTR. Glafenine hydrochloride inhibits the proliferation and clonogenic activity of haSMCs and ECs in a dose-dependent manner. A block in the G2/M phase and a reduction in the G1 phase occurr. The migratory ability of haSMCs is impaired in a dose-dependent manner and the extracellular matrix protein tenascin is reduced.

体内研究

Glafenine injection (25 mg/kg i.v.) shows enhanced BLI signal in mice with an average of 2.9-fold signal enhancement over the control. Glafenine causes increases in BLI signal of up to 11.6- and 17.4-fold in two separate HEK293/ABCG2/fLuc xenografts in the same mouse compared to the signals generated by those xenografts immediately before injection. Incubating polarized CFBE41o     ^-    monolayers and intestines isolated from mutant CFTR mice with glafenine increases the short-circuit current response to forskolin and genistein. Treatment with glafenine also partially restores total salivary secretion. Glafenine-treated zebrafish shows evidence of endoplasmic reticulum and mitochondrial stress, with disrupted intestinal architecture and halted cell stress responses, alongside accumulation of apoptotic intestinal epithelial cells in the lumen.

安全信息

MSDS信息

格拉非宁 盐酸盐 上下游产品信息