2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2

生物活性靶点体外研究体内研究 2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2 试剂级价格

CAS号:729589-58-6
英文名:2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
中文名:2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2
CBNumber:CB1382037
分子式:C36H63N11O8
分子量:777.95
MOL File:729589-58-6.mol

2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2化学性质

密度 :1.33±0.1 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :Soluble in H2O
形态 :powder
酸度系数(pKa) :12.91±0.46(Predicted)
颜色 :white
水溶解性 :Soluble to 1 mg/ml in water

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26
WGK Germany :3

2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2性质、用途与生产工艺

生物活性 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。
靶点

Proteinase-activated receptor 2 (PAR2)
体外研究

2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH ₂ ) is equally effective to and 10 to 25 times more potent than SLIGRLNH ₂ 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-NH ₂ ) is 10 to 300 times more potent than SLIGRL-NH ₂ . Unlike trans-cinnamoyl-LIGRLO-NH ₂ , 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries.

体内研究

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.

Animal Model:	Adult male (2/3-month-old) Trpv3 ^-/- and WT mice
Dosage:	10 μg
Administration:	Injected intradermally at the nape of the neck
Result:	Was involved in PAR2- induced acute itch.