IS-741

Names

[ Name ]:
IS-741

[Synonym ]:
IS 741
N-(2-((Ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)cyclohexanecarboxamide
Cyclohexanecarboxamide,N-(2-((ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Research Areas >> Inflammation/Immunology

[In Vitro]

Fuzapladib(IS-741)(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(IS-741)(p.o., 50 mg/kg, 7 days) 显着降低了大鼠回肠中的髓过氧化物酶 (MPO) 活性和粘膜 IL-8 水平，减少了多形核细胞和 Mac-1 阳性细胞向发炎病灶的浸润，有效减轻了三硝基苯磺酸(TNBS)诱导的大鼠回肠炎[2]。

[References]

[1]. H Shikama, et al. Effect of IS-741 on Cell Adhesion between Human Umbilical Vein Endothelial Cells and HL-60 Cells.

[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

[ Density]:
1.411g/cm3

[ Molecular Formula ]:
C₁₅H₂₀F₃N₃O₃S

[ Molecular Weight ]:
379.39800

[ Exact Mass ]:
379.11800

[ PSA ]:
100.03000

[ LogP ]:
5.18410

[ Index of Refraction ]:
1.548

Related Compounds

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