2014368-93-3
2014368-93-3 structure
- Name: I-287
- Chemical Name: I-287
- CAS Number: 2014368-93-3
- Molecular Formula: C30H30ClFN4O4
- Molecular Weight: 565.042
- Catalog: Signaling Pathways GPCR/G Protein Protease-Activated Receptor (PAR)
- Create Date: 2022-07-01 12:44:27
- Modify Date: 2024-01-09 20:13:26
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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.
| 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. |
|---|---|
| References | 1. Avet C, et al. Commun Biol. 2020 Nov 27;3(1):719. |
| Molecular Formula | C30H30ClFN4O4 |
|---|---|
| Molecular Weight | 565.042 |