Fuzapladib sodium

Modify Date: 2024-01-16 06:36:48

Fuzapladib sodium Structure
Fuzapladib sodium structure
Common Name Fuzapladib sodium
CAS Number 141284-73-3 Molecular Weight 401.38000
Density N/A Boiling Point 522.9ºC at 760mmHg
Molecular Formula C15H19F3N3NaO3S Melting Point N/A
MSDS N/A Flash Point 270.1ºC

 Use of Fuzapladib sodium


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].

 Names

Name sodium,[3-(cyclohexanecarbonylamino)-5-(trifluoromethyl)pyridin-2-yl]-ethylsulfonylazanide
Synonym More Synonyms

 Fuzapladib sodium 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
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

 Synonyms

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