Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
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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 (0-60 μM; 15-30 minutes) inhibits PAR2-mediated activation of Gαq and Gα12/13 proteins in HEK-293 cells without affecting Gi/o proteins, and does not impact β-arrestin 2 recruitment or receptor internalization [1]. Additionally, I-287 (0-60 μM; 15-30 minutes) suppresses PAR2-mediated ERK1/2 activation [1]. At a concentration of 10 μM for 30 minutes, I-287 also inhibits the secretion of the cytokine IL-8 induced by PAR2 in HCT-116 and A549 cells [1]. |
In vivo | I-287 (orally administered at a dosage of 50 mg/kg) reduced the inflammatory response induced by Complete Freund's adjuvant in C57BL/6J mice [1]. |
Molecular Weight | 565.04 |
Formula | C30H30ClFN4O4 |
CAS No. | 2014368-93-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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I-287 2014368-93-3 inhibitor inhibit