141284-73-3

141284-73-3 structure

Name: Fuzapladib sodium
Chemical Name: sodium,[3-(cyclohexanecarbonylamino)-5-(trifluoromethyl)pyridin-2-yl]-ethylsulfonylazanide
CAS Number: 141284-73-3
Molecular Formula: C₁₅H₁₉F₃N₃NaO₃S
Molecular Weight: 401.38000
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2016-09-09 06:19:33
Modify Date: 2024-01-16 06:36:48
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].

Name	sodium,[3-(cyclohexanecarbonylamino)-5-(trifluoromethyl)pyridin-2-yl]-ethylsulfonylazanide
Synonyms	N-(2-(Ethylsulfonamido)-5-(trifluoromethyl)-3-pyridinyl)cyclohexanecarboxamide sodium salt Cyclohexanecarboxamide,N-(2-((ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)-,monosodium salt

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.