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65513-72-6

中文名稱 格拉非寧 鹽酸鹽
英文名稱 1-GLYCERYL N-[7-CHLORO-4-QUINOLYL]ANTHRANILATE HYDROCHLORIDE
CAS 65513-72-6
分子式 C19H18Cl2N2O4
分子量 409.26
MOL 文件 65513-72-6.mol
65513-72-6 結構式 65513-72-6 結構式

基本信息

中文別名
格拉非寧 鹽酸鹽
英文別名
GlafenineHCl
Glafenin hydrochloride
GLAFENINE HYDROCHLORIDE
1-GLYCERYL N-[7-CHLORO-4-QUINOLYL]ANTHRANILATE HYDROCHLORIDE
所屬類別
分析化學:分析標準品

物理化學性質

儲存條件Inert atmosphere,Room Temperature
溶解度DMSO : ≥ 60 mg/mL (146.61 mM)
形態(tài)neat
顏色Light yellow to yellow

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
危險品標志Xn
危險類別碼22
安全說明36
WGK Germany3
RTECS號CB2687000

常見問題列表

生物活性
Glafenine hydrochloride 是一種非甾體抗炎藥 (NSAID), 具有鎮(zhèn)痛活性。
靶點

IC50: 3.2 μM (ABCG2)

體外研究

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.

體內研究

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.

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