KP496

• CAT Number: I020577
• CAS Number: 217799-03-6
• Molecular Formula: C₃₁H₃₄ClN₃O₇S₃
• Molecular Weight: 692.27
• Purity: ≥95%
• Target: Leukotriene Receptor
• IUPAC Name: 2-[4-[(4-chlorophenyl)sulfonylamino]butyl-[[3-[(4-propan-2-yl-1,3-thiazol-2-yl)methoxy]phenyl]methyl]sulfamoyl]benzoic acid
• InChI: InChI=1S/C31H34ClN3O7S3/c1-22(2)28-21-43-30(34-28)20-42-25-9-7-8-23(18-25)19-35(45(40,41)29-11-4-3-10-27(29)31(36)37)17-6-5-16-33-44(38,39)26-14-12-24(32)13-15-26/h3-4,7-15,18,21-22,33H,5-6,16-17,19-20H2,1-2H3,(H,36,37)
• InChIKey: WMMCMKVGDPXYQS-UHFFFAOYSA-N
• SMILES: CC(C)C1=CSC(=N1)COC2=CC=CC(=C2)CN(CCCCNS(=O)(=O)C3=CC=C(C=C3)Cl)S(=O)(=O)C4=CC=CC=C4C(=O)O

KP496(CAT: I020577) is a selective, dual antagonist targeting the Leukotriene D4 receptor and Thromboxane A2 receptor, with significant potential in managing inflammatory conditions. Preclinical studies highlight its effectiveness in reducing acute (day 7) and chronic (day 21) lung inflammation. KP496 notably attenuates lymphocyte counts on day 7 and macrophages, neutrophils, and eosinophils on days 7 and 21. It significantly suppresses the elevation of hydroxyl-L-proline content in the lung, achieving a 74% inhibition ratio compared to 63% by prednisolone. At doses of 100 mg/head, KP496 demonstrates superior inhibition of infiltrating total cells, eosinophils, monocytes/macrophages, and lymphocytes compared to control groups, suggesting robust anti-inflammatory properties and potential as a therapeutic agent in chronic inflammatory conditions.

Reference

[1]. Kurokawa S, et al. Effect of inhaled KP-496, a novel dual antagonist of the cysteinyl leukotriene and thromboxane A2 receptors, on a bleomycin-induced pulmonary fibrosis model in mice. Pulm Pharmacol Ther. 2010 Oct;23(5):425-31.[2]. Ishimura M, et al. Effects of KP-496, a novel dual antagonist for cysteinyl leukotriene receptor 1 and thromboxane A2 receptor, on Sephadex-induced airway inflammation in rats. Biol Pharm Bull. 2009 Jun;32(6):1057-61.