KP496
KP496 Basic information
- Product Name:
- KP496
- Synonyms:
-
- KP496
- Benzoic acid, 2-[[[4-[[(4-chlorophenyl)sulfonyl]amino]butyl][[3-[[4-(1-methylethyl)-2-thiazolyl]methoxy]phenyl]methyl]amino]sulfonyl]-
- KP496,KP-496
- CAS:
- 217799-03-6
- MF:
- C31H34ClN3O7S3
- MW:
- 692.27
- Mol File:
- 217799-03-6.mol
KP496 Chemical Properties
- Boiling point:
- 847.9±75.0 °C(Predicted)
- Density
- 1.378±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 3.09±0.36(Predicted)
- color
- White to off-white
KP496 Usage And Synthesis
Uses
KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
in vivo
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].
IC 50
LTD4; TXA2 Receptor
References
[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. DOI:10.1016/j.pupt.2010.04.008
[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. DOI:10.1248/bpb.32.1057
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