2-Furoyl-LIGRLO-amide

发表于由

2-Furoyl-LIGRLO-amide; 纯度: 99.55%

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。

2-Furoyl-LIGRLO-amideamp;;

2-Furoyl-LIGRLO-amide Chemical Structure

CAS No. : 729589-58-6

规格 价格 是否有货 数量
1 mg ￥1200 In-stock
5 mg ￥3600 In-stock
10 mg ￥6120 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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2-Furoyl-LIGRLO-amide 相关产品

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生物活性

2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value 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 SLIGRLNH2 for 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

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
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. McGuire JJ, et al. 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J Pharmacol Exp Ther. 2004 Jun;309(3):1124-31.

    [2]. Lohman RJ, et al. An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. FASEB J. 2012 Jul;26(7):2877-87.

    [3]. Jiahui Zhao, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol