Glafenine (hydrochloride)

Glafenine (Glafenin) hydrochloride is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine hydrochloride exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine hydrochloride can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine hydrochloride can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF)^[1][2][3][4]. In Vitro:Glafenine hydrochloride (10-100 μM; 4-20 days) inhibits cell proliferation and colony formation in human aortic smooth muscle cells (haSMCs) and endothelial cells (ECs) in a dose-dependent manner, induces cell cycle arrest at the G2/M phase, and reduces the synthesis of the extracellular matrix protein tenascin^[1].
Glafenine hydrochloride (10 μM; 24 h) promotes the maturation and translocation of the F508del-CFTR mutant protein to the cell surface and enhances its chloride channel function in human bronchial epithelial cells (HBE) by inhibiting the COX-2-mediated arachidonic acid pathway^[2]. In Vivo:Glafenine hydrochloride (25 μM; immersion; single; 12 h) induces intestinal epithelial cell apoptosis, endoplasmic reticulum (ER) and mitochondrial stress, and damages intestinal structure in zebrafish larvae, while the μ-opioid receptor agonist DALDA (HY-P3870) alleviates the intestinal damage induced by glafenine by enhancing the atf6-dependent unfolded protein response (UPR)^[3].