So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Avet, Charlotte; Sturino, Claudio; Grastilleur, Sebastien; Gouill, Christian Le; Semache, Meriem; Gross, Florence; Gendron, Louis; Bennani, Youssef; Mancini, Joseph A.; Sayegh, Camil E.; Bouvier, Michel researched the compound: Methyl 6-bromonicotinate( cas:26218-78-0 ).Safety of Methyl 6-bromonicotinate.They published the article 《The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signalling and has anti-inflammatory effects》 about this compound( cas:26218-78-0 ) in Communications Biology. Keywords: protease activated receptor inhibitor signalling antiinflammatory effect. We’ll tell you more about this compound (cas:26218-78-0).
Protease-activated receptor-2 (PAR2) is involved in inflammatory responses and pain, therefore representing a promising therapeutic target for the treatment of immune-mediated inflammatory diseases. However, as for other GPCRs, PAR2 can activate multiple signaling pathways and those involved in inflammatory responses remain poorly defined. Here, we describe a new selective and potent PAR2 inhibitor (I-287) that shows functional selectivity by acting as a neg. allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors, while having no effect on Gi/o signaling and βarrestin2 engagement. Such selective inhibition of only a subset of the pathways engaged by PAR2 was found to be sufficient to block inflammation in vivo. In addition to unraveling the PAR2 signaling pathways involved in the pro-inflammatory response, our study opens the path toward the development of new functionally selective drugs with reduced liabilities that could arise from blocking all the signaling activities controlled by the receptor.
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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem