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Fuzapladib sodium

Names

[ CAS No. ]:
141284-73-3

[ Name ]:
Fuzapladib sodium

[Synonym ]:
N-(2-(Ethylsulfonamido)-5-(trifluoromethyl)-3-pyridinyl)cyclohexanecarboxamide sodium salt
Cyclohexanecarboxamide,N-(2-((ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)-,monosodium salt

Biological Activity

[Description]:

Fuzapladib sodium (IS-741 sodium) is a potent and orally active phospholipase A2 inhibitor. Fuzapladib sodium can block the adhesion of inflammatory cells to microvascular endothelial cells, inhibits the infiltration of neutrophils into the pancreas or acute pancreatitis, and has anti-acute pancreatitis effects[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase
Research Areas >> Inflammation/Immunology

[In Vitro]

Fuzapladib sodium (IS-741 sodium)(1 μM, 3 h) 在脂多糖刺激下，可显着抑制 HL-60 细胞与 HUVEC 的粘附[1]。

[In Vivo]

Fuzapladib sodium (IS-741 sodium) (p.o., 50 mg/kg, 7 days) 抑制中性粒细胞浸润炎性病变，对减轻大鼠TNBS回肠炎有效[2]。 Animal Model: Rats[2] Dosage: 50 mg/kg Administration: P.o.; for 7 days Result: Significantly reduced myeloperoxidase (MPO) activity and mucosal IL-8 levels in rat ileum, reduced polymorphonuclear cells and Mac-1 positivity Infiltration of cells into inflammatory lesions, effectively alleviated trinitrobenzenesulfonic acid (TNBS)-induced ileitis.

[References]

[1]. Shikama H, et al. Effect of IS-741 on cell adhesion between human umbilical vein endothelial cells and HL-60 cells. Biol Pharm Bull. 1999 Feb;22(2):127-31.  

[2]. Tetsuya Fukunaga, et al. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9.  

Chemical & Physical Properties

[ Boiling Point ]:
522.9ºC at 760mmHg

[ Molecular Formula ]:
C15H19F3N3NaO3S

[ Molecular Weight ]:
401.38000

[ Flash Point ]:
270.1ºC

[ Exact Mass ]:
401.10000

[ PSA ]:
84.51000

[ LogP ]:
5.12790

[ Vapour Pressure ]:
9.19E-12mmHg at 25°C

Related Compounds