| Bioactivity | I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research[1]. |
| Invitro | I-287 (0-60 μM; 15-30 分钟) 抑制在 HEK-293 细胞中 PAR2 介导的 Gαq 和 Gα12/13 而不是 Gi/o 蛋白的激活，而对 PAR2 介导的 β arrestin 2 募集和受体内化没有影响[1]。I-287 (0-60 μM; 15-30 分钟) 抑制 PAR2 介导的 ERK1/2 激活[1]。I-287 (10 μM；30 分钟) 可抑制 HCT-116 和 A549 细胞中 PAR2 诱导的 IL-8 细胞因子的分泌[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | I-287(口服，50 mg/kg) 降低 C57BL/6J 小鼠中 Complete Freund's adjuvant (HY-153808) 诱导的炎症反应[1]。 Animal Model: |
| Name | I-287 |
| CAS | 2014368-93-3 |
| Formula | C30H30ClFN4O4 |
| Molar Mass | 565.04 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Avet C, et.al. The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signaling and has anti-inflammatory effects. Commun Biol. 2020 Nov 27;3(1):719. |