格拉非宁 盐酸盐
中文名称 | 格拉非宁 盐酸盐 |
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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 | GLAFENINE HYDROCHLORIDE;1-GLYCERYL N-[7-CHLORO-4-QUINOLYL]ANTHRANILATE HYDROCHLORIDE;GlafenineHCl;Glafenin 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
储存条件 | Inert atmosphere,Room Temperature |
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溶解度 | 二甲基亚砜:≥ 60 mg/mL(146.61 mM) |
形态 | 固体 |
颜色 | 浅黄至黄色 |
IC50: 3.2 μM (ABCG2)
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.
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.
提供商 | 语言 |
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英文
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