| Description | I-287 is a selective, orally active PAR2 inhibitor that functions as a negative allosteric modulator of Gαq and Gα12/13 activity and their downstream effectors. It has been shown to attenuate Complete Freund's adjuvant-induced inflammation in mice, suggesting its utility in inflammation/immunology research [1]. |
| In vitro | I-287在0-60μM浓度范围内，处理时间15-30分钟，在HEK-293细胞中特异性抑制了PAR2介导的Gαq和Gα12/13蛋白激活，而不影响G i/o蛋白或β arrestin 2的募集及受体内化[1]。此外，I-287在同样条件下抑制了PAR2介导的ERK1/2信号通路的激活[1]。在10μM浓度、30分钟处理时，还能够抑制HCT-116和A549细胞中由PAR2诱导的IL-8细胞因子的分泌[1]。 |
| In vivo | I-287(口服，50 mg/kg)显著抑制了C57BL/6J小鼠中Complete Freund's adjuvant所引起的炎症[1]。 |
| molecular weight | 565.04 |
| Molecular formula | C30H30ClFN4O4 |
| CAS | 2014368-93-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |