2-Furoyl-LIGRLO-amide TFA 

2-Furoyl-LIGRLO-amide TFA is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD₂ value of 7.0^[1][2]..

2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH₂) is equally effective to and 10 to 25 times more potent than SLIGRLNH₂ for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively^[1].
In bioassays of tissue PAR2 activity, measured as arterial vasodilation and hyperpolarization, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH₂) is 10 to 300 times more potent than SLIGRL-NH₂. Unlike trans-cinnamoyl-LIGRLO-NH₂, 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Furoyl-LIGRLO-amide TFA (injected intradermally at the nape of the neck; 10 μg; pre-injected) exhibits fewer scratches in response to 2-Furoyl-LIGRLO-amide but not to histamine in Trpv3^-/- mice. But it decreases significantly the number of scratches in WT mice^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

891.98

C₃₈H₆₄F₃N₁₁O₁₀

2468029-34-5

{Fur-2-oyl}-Leu-Ile-Gly-Arg-Leu-{Orn}-NH2

{Fur-2-oyl}-LIGRL-{Orn}-NH2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. McGuire JJ, et al. 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J Pharmacol Exp Ther. 2004 Jun;309(3):1124-31.  [Content Brief]

  [2]. Lohman RJ, et al. An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. FASEB J. 2012 Jul;26(7):2877-87.  [Content Brief]

  [3]. Jiahui Zhao, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol  [Content Brief]