I-287
Modify Date: 2025-08-25 13:47:14
I-287 structure
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Common Name | I-287 | ||
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| CAS Number | 2014368-93-3 | Molecular Weight | 565.042 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C30H30ClFN4O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of I-287I-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. |
| Name | I-287 |
|---|
| 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. |
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| References | 1. Avet C, et al. Commun Biol. 2020 Nov 27;3(1):719. |
| Molecular Formula | C30H30ClFN4O4 |
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| Molecular Weight | 565.042 |