IS 741
- Product Name
- IS 741
- CAS No.
- 141283-87-6
- Chemical Name
- IS 741
- Synonyms
- IS 741;Fuzapladib;IS-741 (Fuzapladib;Fuzapladib （IS-741）;Fuzapladib, 10 mM in DMSO;N-(2-(Ethylsulfonamido)-5-(trifluoromethyl)pyridin-3-yl)cyclohexanecarboxamide;Cyclohexanecarboxamide, N-[2-[(ethylsulfonyl)amino]-5-(trifluoromethyl)-3-pyridinyl]-
- CBNumber
- CB61364116
- Molecular Formula
- C15H20F3N3O3S
- Formula Weight
- 379.4
- MOL File
- 141283-87-6.mol
IS 741 Property
- Density
- 1.411±0.06 g/cm3(Predicted)
- storage temp.
- -10 to -25°C
- solubility
- DMSO: 2mg/mL, clear
- pka
- 5.41±0.10(Predicted)
- form
- Solid
- 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
IS 741 Chemical Properties,Usage,Production
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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