I-287
Names
[ CAS No. ]:
2014368-93-3
[ Name ]:
I-287
Biological Activity
[Description]:
I-287 is a potent, selective, orally active inhibitor of PAR2, negative PAR2 allosteric modulator, inhibits PAR2-mediated activation of Gq and G12/13 but not Gi/o proteins (IC50=45-390 nM);I-287 is a negative allosteric modulator (NAM) and not an orthosteric competitive antagonist of hPAR2.I-287 inhibits PAR2-mediated activation of DAG/Ca2+/PKC and RhoA/SRF-RE, as well as FAK and ERK1/2 signaling pathways, shows no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization.I-287 inhibits PAR2-induced secretion of IL-8 cytokine in vitro and reduces Freund's adjuvant (CFA)-induced paw edema model in mice.
[References]
1. Avet C, et al. Commun Biol. 2020 Nov 27;3(1):719.
Chemical & Physical Properties
[ Molecular Formula ]:
C30H30ClFN4O4
[ Molecular Weight ]:
565.042