KP496 

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

KP496 significantly inhibits acute (day 7) and chronic (day 21) lung inflammation. KP496 attenuates the number of lymphocytes on day 7 and those of macrophages, neutrophils, and eosinophils on days 7 and 21. KP496 and prednisolone significantly suppress the increase of hydroxyl-L-proline content in the lung. Compare to respective vehicle control group, the inhibition ratio of KP496 and prednisolone for increase of hydroxyl-L-proline content is about 74 and 63%, respectively^[1]. The KP496 (100 mg/head) group and prednisolone (10 mg/kg) group exhibit significant inhibition of numbers of infiltrating total cells, eosinophils, monocytes/macrophages, and lymphocytes compare with the control group. Infiltration of all types of cells except neutrophils is decreased in the KP496 (30m g/head) group, though not to significant extents^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

692.27

Solid

C₃₁H₃₄ClN₃O₇S₃

217799-03-6

O=C(O)C1=CC=CC=C1S(=O)(N(CCCCNS(=O)(C2=CC=C(Cl)C=C2)=O)CC3=CC=CC(OCC4=NC(C(C)C)=CS4)=C3)=O

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]