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Glafenine hydrochloride

CAS No. : 65513-72-6

MCE 站：Glafenine hydrochloride

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

研究领域：Others

作用靶点：Others

In Vitro: 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.

In Vivo: 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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