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(2-Furoyl)-PAR-2 (2-6)-Orn amide (mouse, rat)

CAS No.: 729589-58-6

(2-Furoyl)-PAR-2 (2-6)-Orn amide (mouse, rat) also called (2-Furoyl)-LIGRLOamide, 2-Furoyl-LIGRLO-NH2 Potent and Selecti
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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