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CAS No. : 729589-58-6
MCE 国际站:2-Furoyl-LIGRLO-amide
产品活性:2-Furoyl-LIGRLO-amide 是一种有效的选择性蛋白酶激活受体2 (PAR2) 激动剂, 其 pD2 值为 7.0。
研究领域:GPCR/G Protein
作用靶点:Protease Activated Receptor (PAR)
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.
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.
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.
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