Glafenine hydrochloride

• CAT Number: I013505
• CAS Number: 65513-72-6
• Molecular Formula: C₁₉H₁₈Cl₂N₂O₄
• Molecular Weight: 409.26
• Purity: ≥95%
• Target: Others
• Solubility: DMSO: ≥60 mg/mL
• IUPAC Name: 2,3-dihydroxypropyl 2-[(7-chloroquinolin-4-yl)amino]benzoate;hydrochloride
• InChI: InChI=1S/C19H17ClN2O4.ClH/c20-12-5-6-14-17(7-8-21-18(14)9-12)22-16-4-2-1-3-15(16)19(25)26-11-13(24)10-23;/h1-9,13,23-24H,10-11H2,(H,21,22);1H
• InChIKey: CEUMONXVSJOJIH-UHFFFAOYSA-N
• SMILES: C1=CC=C(C(=C1)C(=O)OCC(CO)O)NC2=C3C=CC(=CC3=NC=C2)Cl.Cl

Glafenine hydrochloride (CAT: I013505) serves as a non-narcotic analgesic and non-steroidal anti-inflammatory drug (NSAID). Its pharmacological action involves alleviating pain and reducing inflammation through mechanisms such as inhibition of prostaglandin synthesis. Additionally, Glafenine hydrochloride functions as an ABCG2 inhibitor, with an IC50 of 3.2 μM. This inhibition impacts the function of the ABCG2 transporter protein, which plays a role in drug efflux and cellular detoxification.

Reference

[1]. Zhang Y, et al. Identification of inhibitors of ABCG2 by a bioluminescence imaging-based high-throughput assay. Cancer Res. 2009 Jul 15;69(14):5867-75. [2]. Robert R, et al. Correction of the Delta phe508 cystic fibrosis transmembrane conductance regulator trafficking defect by the bioavailable compound glafenine. Mol Pharmacol. 2010 Jun;77(6):922-30. [3]. Schöber W, et al. Impact of glafenine hydrochloride on human endothelial cells and human vascular smooth muscle cells: a substance reducing proliferation, migration and extracellular matrix synthesis. Cell Biol Int. 2003;27(12):987-96.[4]. Goldsmith JR, et al. Glafenine-induced intestinal injury in zebrafish is ameliorated by μ-opioid signaling via enhancement of Atf6-dependent cellular stress responses. Dis Model Mech. 2013 Jan;6(1):146-59.