| Identification | Back Directory | [Name]
IS 741 | [CAS]
141283-87-6 | [Synonyms]
IS 741
Fuzapladib
Fuzapladib （IS-741）
IS-741
(Fuzapladib
Cyclohexanecarboxamide, N-[2-[(ethylsulfonyl)amino]-5-(trifluoromethyl)-3-pyridinyl]- | [Molecular Formula]
C15H20F3N3O3S | [MOL File]
141283-87-6.mol | [Molecular Weight]
379.4 |
| Chemical Properties | Back Directory | [density ]
1.411±0.06 g/cm3(Predicted) | [storage temp. ]
-10 to -25°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
5.41±0.10(Predicted) | [color ]
White to off-white | [InChI]
InChI=1S/C15H20F3N3O3S/c1-2-25(23,24)21-13-12(8-11(9-19-13)15(16,17)18)20-14(22)10-6-4-3-5-7-10/h8-10H,2-7H2,1H3,(H,19,21)(H,20,22) | [InChIKey]
TUWCZRFHNIOVTC-UHFFFAOYSA-N | [SMILES]
C1(C(NC2=CC(C(F)(F)F)=CN=C2NS(CC)(=O)=O)=O)CCCCC1 |
| Hazard Information | Back Directory | [Uses]
Fuzapladib (IS-741), an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site[1][2]. | [Biological Activity]
Fuzapladib (IS-741) is a cell penetrant and potent phospholipase A2 (PLA2) inhibitor. Fuzapladib decelerate the progression of pancreatic fibrosis through monocyte infiltration in dogs. | [in vivo]
Fuzapladib (IS-741) (p.o., 50 mg/kg, 7 days) inhibits neutrophil infiltration into inflamed lesions, and is effective for attenuating rat trinitrobenzene sulfonic acid (TNBS) ileitis[4]. | Animal Model: | Rats[4] | | 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] Noriyuki Kaji, et al. Fuzapladib reduces postsurgical inflammation in the intestinal muscularis externa. J Vet Med Sci. 2023 Sep 21. DOI:10.1292/jvms.23-0257
[2] C Bassi. IS-741 (Ishihara Sangyo). Curr Opin Investig Drugs. 2001 Apr;2(4):510-2. PMID:11566008
[3] 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. DOI:10.1248/bpb.22.127
[4] 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. DOI:10.1007/s00535-002-1081-8 |
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