2-Furoyl-LIGRLO-amide TFA

发表于由

2-Furoyl-LIGRLO-amide TFA;

2-Furoyl-LIGRLO-amide TFA 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-amide TFAamp;;

2-Furoyl-LIGRLO-amide TFA Chemical Structure

规格 价格 是否有货
1 mg ￥1200 询问价格 货期
5 mg ￥3600 询问价格 货期
10 mg ￥6120 询问价格 货期

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2-Furoyl-LIGRLO-amide TFA 的其他形式现货产品:

2-Furoyl-LIGRLO-amide

生物活性

2-Furoyl-LIGRLO-amide TFA 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 TFA (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[3].

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[2]
Dosage: 10 μg
Administration: Injected intradermally at the nape of the neck
Result: Was involved in PAR2- induced acute itch.

分子量

891.98

Formula

C38H64F3N11O10
Sequence

{Fur-2-oyl}-Leu-Ile-Gly-Arg-Leu-{Orn}-NH2
Sequence Shortening

{Fur-2-oyl}-LIGRL-{Orn}-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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