PAR-1 agonist/ TRAP6 TFLLR-amide
Representing the activating sequence of the “tethered ligand” of protease cleaved PAR-1; activates PAR-1 with high selectivity
Catalogue number crb1000217 Molecular Weight 647.8 Sequence (one letter code) TFLLR-amide Sequence (three letter code) H-Thr-Phe-Leu-Leu-Arg-NH2 Molecular Weight 647.8 Purity >95% Storage -20°C References
Zhang et al (2014) Evaluation on Potential Contributions of Protease Activated Receptors Related Mediators in Allergic Inflammation. Mediators Inflamm. 2014 1 PMID: 24876677
Protease activated receptors (PARs) are a distinctive four-member family of seven transmembrane G protein-coupled receptors (GPCRs) widely expressed in inflammatory cells. PARs are cleaved by certain serine proteases to expose a tethered ligand domain, this ligand domain then binds to and activates the receptors to initiate multiple signalling cascades. These PAR-activating proteases therefore represent PAR agonists. This PAR-1 agonist peptide represents the sequence of the “tethered ligand” and is therefore capable of activating the receptor independently of N-terminal proteolysis. TFLLR-NH2 is more selective to PAR-1 than the PAR-1 agonist SFLLRN-NH2.
Activation of PAR-1 induces platelet aggregation and IL-6 release from monocytes and T cells, as well as several other cellular pathways including those involved in allergic inflammation, neurogenic inflammation and the potentiation of NMDA receptor activity in the hippocampus