CAS | 729589-58-6 |
Sequence | (2-Furoyl)-Leu-Ile-Gly-Arg-Leu-Orn-NH2 |
Sequence Single | (2-Furoyl)-LIGRL-Orn-NH2 |
Molecular Formula | C36H63N11O8 |
Molecular Weight | 777.97 |
Synonyms | (2-Furoyl)-LIGRLOamide, 2-Furoyl-LIGRLO-NH2 Potent and Selective Protease-Activated Receptor 2 (PAR2) Agonist |
Technology | Synthetic |
Storage | -20°C, avoid light, cool and dry place |
Application | Cardiovascular System & Diseases|Hematology |
Description | (2-Furoyl)-PAR-2 (2-6)-Orn amide (mouse, rat) also called (2-Furoyl)-LIGRLOamide, 2-Furoyl-LIGRLO-NH2 Potent and Selective Protease-Activated Receptor 2 (PAR2) Agonist, is a potent and selective PAR-2 agonist with a pD2 value of 7.0. In cultured human PAR-2-expressing cells (2-Furoyl)-PAR-2 (2-6)-Orn amide was equally effective as SLIGRL-amide, in rat PAR-2-expressing cells it was 10 to 25 times more potent than SLIGRLamide in increasing intracellular calcium levels. In bioassays of tissue PAR-2 activity, measured as arterial vasodilation and hyperpolarization this agonist was 10 to 300 times more potent than SLIGRL-amide. |
References | 1. Serpin1 of Arabidopsis thaliana is a suicide inhibitor for metacaspase 9. D.Vercammen et al., J. Mol. Biol., 364, 625 (2006) 2. 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J.J.McGuire et al., J. Pharmacol. Exp. Ther., 309, 1124 (2004) 3. An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. Lohman RJ, et al. FASEB J. 2012 Jul;26(7):2877-87. 4. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. Jiahui Zhao, et al. J Invest Dermatol |