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VKGILS-NH2 Sale

(Synonyms: 蛋白酶激活的受体2(PAR2)激动剂对照多肽) 目录号 : GC11727

VKGILS-NH2 是 SLIGKV-NH2(蛋白酶激活受体 2 (PAR2) 激动剂)的反向氨基酸序列控制肽。

VKGILS-NH2 Chemical Structure

Cas No.:942413-05-0

规格 价格 库存 购买数量
5 mg
¥1,080.00
现货
10 mg
¥1,800.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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VKGILS-NH2 serves as the reversed amino acid sequence control peptide for SLIGKV-NH2, a protease-activated receptor 2 (PAR2) agonist. PARs are a group of G-protein-coupled receptors existing in several cell types. Up to date, four PAR members including PAR1 to 4 have been identified, cloned and designated. PAR2 is expressed in the respiratory and gastrointestinal tracts. It is suggested that the activation of PAR2 is closely correlated with inflammatory evens in various cells and tissues. PAR2 has also been identified to induce protease activation and therefore result in systemic hypotension. [1]

In vitro: The PAR2 activating peptide AP (SLIGKV-NH2) and the reverse peptide control RP (VKGILS-NH2) were used in one study to reveal that PAR2 slightly enhanced mucin secretion by human bronchial epithelial cells in vitro. According to this study, compared to cells treated with VKGILS-NH2, exposure of cells to the synthetic PAR2 agonist peptide (SLIGKV-NH2) for 30 mins resulted in a weak but statistically significant increase in mucin secretion at concentrations of 100 and 1000M. [1]

In vivo: In one in vivo study, the mouse PAR2 reverse (LRGILS-NH2) and human PAR2 reverse (VKGILS-NH2) peptides were adopted as control which caused no contractile responses at the highest concentrations, with the aim to prove in the guinea-pig gallbladder PAR1 and PAR2 activation could lead to contractile responses. [2]

Clinical trial: PAR2 activating peptide, SLIGKV-NH2, and its reverse-sequence control peptide VKGILS-NH2 were synthesized to verify the hypothesis that in vivo activation of PAR2 in humans would cause vasodilatation. The result of this study showed that, in forearm resistance vessels, SLIGKV-NH2 triggered a dose-dependent dilatation, while VKGILS-NH2 had no significant effect. [3]

References:
[1] Lin KW, Park J, Crews AL, Li YH, Adler KB.  Protease-activated receptor-2 (PAR-2) is a weak enhancer of mucin secretion by human bronchial epithelial cells in vitro. Int J Biochem Cell B. 2008. 40: 137988.
[2] Tognetto M, Trevisani M, Maggiore B, Navarra G, Turini A, Guerrini R, Bunnett NW, Geppetti P and Harrison S.  Evidence that PAR-1 and PAR-2 mediate prostanoid-dependent contraction in isolated guinea-pig gallbladder. Br.J.Pharmacol. 2000.131: 689-94.
[3] Robin J, Kharbanda R, Mclean P, Campbell R, Vallance P.  Protease-activated receptor 2–mediated vasodilatation in humans in vivo, role of nitric oxide and prostanoids. Circulation. 2003;107:954-959.

Chemical Properties

Cas No. 942413-05-0 SDF
别名 蛋白酶激活的受体2(PAR2)激动剂对照多肽
化学名 (S,Z)-6-amino-2-((Z)-((S)-2-amino-1-hydroxy-3-methylbutylidene)amino)-N-((Z)-2-(((2S,3S,Z)-1-(((S,Z)-1-(((S)-1,3-dihydroxy-1-iminopropan-2-yl)imino)-1-hydroxy-4-methylpentan-2-yl)imino)-1-hydroxy-3-methylpentan-2-yl)imino)-2-hydroxyethyl)hexanimidic acid
Canonical SMILES CC[C@]([C@@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](N)([H])C(C)C)([H])CCCCN)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CO)([H])CC(C)C)([H])C
分子式 C28H54N8O7 分子量 614.79
溶解度 ≥ 134.4 mg/mL in DMSO, ≥ 13.82 mg/mL in EtOH with ultrasonic and warming, ≥ 62.9 mg/mL in Water 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6266 mL 8.1329 mL 16.2657 mL
5 mM 0.3253 mL 1.6266 mL 3.2531 mL
10 mM 0.1627 mL 0.8133 mL 1.6266 mL
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