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

中文名称:

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

中文同义词:

N-(2-呋喃基羰基)-L-亮氨酰-L-异亮氨酰甘氨酰-L-精氨酰基-L-亮氨酰-L-鸟氨酸酰胺

英文名称:

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

英文同义词:

PAR-2 AGONIST II;PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II;2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2;2-(2-FUROYL)-LIGRLOAMIDE;2-(2-FUROYL)-PAR-2 (2-6)-ORN AMIDE (MOUSE, RAT);2F-LIGRLO-AMIDE;2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2;2-FUROYL-LIGRLO-AMIDE

CAS号:

729589-58-6

分子式:

C36H63N11O8

分子量:

777.95

EINECS号:

相关类别:

多肽

Mol文件:

729589-58-6.mol

储存条件 

-20°C

形态

powder

颜色

white

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.

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.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26

WGK Germany 

3