Powder: -20°C for 3 years | In solvent: -80°C for 1 year
2-Furoyl-LIGRLO-amide TFA is a potent and selective agonist of the proteinase-activated receptor 2 (PAR2), exhibiting a pD2 value of 7.0 [1] [2].
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Description | 2-Furoyl-LIGRLO-amide TFA is a potent and selective agonist of the proteinase-activated receptor 2 (PAR2), exhibiting a pD2 value of 7.0 [1] [2]. |
In vitro | 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) demonstrates equivalent efficacy and exhibits 10 to 25-fold greater potency than SLIGRLNH2 in elevating intracellular calcium levels in human and rat cells expressing PAR2, respectively [1]. Further, when assessing PAR2 activation in tissue, evidenced by arterial vasodilation and hyperpolarization, this compound outperforms SLIGRL-NH2 by a factor of 10 to 300. Contrary to trans-cinnamoyl-LIGRLO-NH2, 2-Furoyl-LIGRLO-amide does not induce significant non-PAR2-mediated contraction in mouse femoral arteries [1]. |
In vivo | When administered intradermally at the nape of the neck as a pre-injection at a dose of 10 μg, Furoyl-LIGRLO-amide TFA reduces scratching responses to 2-Furoyl-LIGRLO-amide in Trpv3 -/- mice, but not to histamine. In wild-type (WT) mice, however, the compound significantly decreases scratch behavior [3]. |
Molecular Weight | 891.98 |
Formula | C38H64F3N11O10 |
CAS No. | 2468029-34-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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2-Furoyl-LIGRLO-amide TFA 2468029-34-5 inhibitor inhibit