2-Furoyl-LIGRLO-amide

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

729589-58-6

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。

生物活性

2-Furoyl-LIGRLO-amide is a potent and selectiveproteinase-activated receptor 2 (PAR2)agonist with apD₂value of 7.0^[1]^[2]..

IC₅₀& Target

Proteinase-activated receptor 2 (PAR2)^[1]

体外研究
(In Vitro)

2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH₂) is equally effective to and 10 to 25 times more potent than SLIGRLNH₂for 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].

体内研究
(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].

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

分子量

777.95

性状

Solid

Formula

C₃₆H₆₃N₁₁O₈

CAS 号

729589-58-6

Sequence Shortening

{Fur-2-oyl}-LIGRL-{Orn}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 50 mg/mL(64.27 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.2854 mL	6.4271 mL	12.8543 mL
5 mM	0.2571 mL	1.2854 mL	2.5709 mL
10 mM	0.1285 mL	0.6427 mL	1.2854 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (64.27 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。