Lodoxamide

Lodoxamide is a potent agonist of GPR35 with an EC50 value of 1.61 nM in a beta-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor. It inhibits histamine release induced by compound 48/80 (Cay-22173), anti-IgE, or A23187 (Cay-11016) in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM) and inhibits A23187-induced calcium influx in mast cells. It reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml. Lodoxamine (0.1 and 10%, w/v) reduces the immediate hypersensitivity response in rat conjunctiva in vivo in a dose-dependent manner and reduces mast cell degranulation in a topical ovalbumin challenge. Formulations containing lodoxamide have been used in the treatment of vernal conjunctivitis and keratitis.Formal Name: 2,2'-[(2-chloro-5-cyano-1,3-phenylene)diimino]bis[2-oxo-acetic acid]. CAS Number: 53882-12-5. Molecular Formula: C11H6ClN3O6. Formula Weight: 311.6. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, PBS (pH 7.2): 2 mg/mL. SMILES: ClC1=C(NC(C(O)=O)=O)C=C(C#N)C=C1NC(C(O)=O)=O. InChi Code: InChI=1S/C11H6ClN3O6/c12-7-5(14-8(16)10(18)19)1-4(3-13)2-6(7)15-9(17)11(20)21/h1-2H,(H,14,16)(H,15,17)(H,18,19)(H,20,21). InChi Key: RVGLGHVJXCETIO-UHFFFAOYSA-N.