2-Furoyl-LIGRLO-amide


CAS No. : 729589-58-6

729589-58-6
Price and Availability of CAS No. : 729589-58-6
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Cat. No. : HY-P1314
M.Wt: 777.95
Formula: C36H63N11O8
Purity: >98 %
Solubility: H2O : 50 mg/mL (ultrasonic)
Introduction of 729589-58-6 :

2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0[1][2].. IC50 & Target:Proteinase-activated receptor 2 (PAR2)[1] In Vitro: 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]. In Vivo: Furoyl-LIGRLO-amide (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[1].

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