| Description | Fuzapladib (IS-741) (IS-741) is a phospholipase A2 inhibitor that can inhibits the expression of Mac-1, a cell adhesion molecule. Fuzapladib blocks activation of adhesion molecules (integrin) expressed on the inflammatory cell surface to prevent inflammatory cells from adhering to vascular endothelial cells and infiltrating tissue and to control exacerbation of pancreatitis. |
| In vitro | 处理Fuzapladib(IS-741) 1μM 3小时显著抑制了由脂多糖刺激后HL-60细胞对HUVEC的黏附[1]。 |
| In vivo | 经口给药Fuzapladib(IS-741) 50mg/kg显著降低了大鼠连续7天小肠myeloperoxidase (MPO)活性及IL-8水平，减少了炎症病灶多核细胞和Mac-1阳性细胞的浸润，并有效缓解了三硝基苯磺酸(TNBS)诱导的小肠炎[2]。 |
| Synonyms | IS-741 |
| molecular weight | 379.4 |
| Molecular formula | C15H20F3N3O3S |
| CAS | 141283-87-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 3.79 mg/mL (10 mM) |
| 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. Fukunaga T, et al. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9. |