SLIGKV-NH2
(Synonyms: 蛋白酶活化的受体-2，酰胺) 目录号 : GC14540
SLIGKV-NH2 (SLIGKV-NH2) 是一种高效的蛋白酶激活受体 2 (PAR2) 激活肽。
Cas No.:190383-13-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
IC50: A protease-activated receptor 2 (PAR2) agonist with an IC50 of 10.4 M.
SLIGKV-NH2 serves as 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: It was reported that SLIGKV-NH2 (the PAR2 activating peptide), by inducing express of PAR2, could slightly enhanced mucin secretion by human bronchial epithelial cells in vitro. According to this study, compared to cells treated with a control peptide with reversed amino acid sequence, exposure of cells to SLIGKV-NH2 for 30 mins resulted in a weak but statistically significant increase in mucin secretion at concentrations of 100 and 1000M. In addition, SLIGKV-NH2 was demonstrated to accelerate cell cycle progression and stimulate the growth of HepG2 cells. [1, 2]
In vivo: The ability of PAR2 agonists to induce contractile responses was investigated in vivo. It was found that mouse PAR2 activating (SLIGRL-NH2) and human PAR2 activating (SLIGKV-NH2) peptides triggered a concentration-dependent contractile response in guinea-pig gallbladder. [3]
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. [4]
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]Xie L, Zheng Y, Li X, Zhao JY, Chen XY, Chen L, Zhou J, Hai O and Li F. Enhanced proliferation of human hepatoma cells by PAR-2 agonists via the ERK/AP-1 pathway. Oncol Rep. 2012.28: 1665-72.
[3] 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.
[4] 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.
| Cas No. | 190383-13-2 | SDF | |
| 别名 | 蛋白酶活化的受体-2，酰胺 | ||
| 化学名 | (2S)-6-amino-2-[[2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-N-[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]hexanamide | ||
| Canonical SMILES | CCC(C)C(C(=O)NCC(=O)NC(CCCCN)C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CO)N | ||
| 分子式 | C28H54N8O7 | 分子量 | 614.78 |
| 溶解度 | ≥ 62.9 mg/mL in DMSO, ≥ 13.48 mg/mL in EtOH with ultrasonic and warming, ≥ 66.2 mg/mL in Water | 储存条件 | Desiccate at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6266 mL | 8.133 mL | 16.266 mL |
| 5 mM | 0.3253 mL | 1.6266 mL | 3.2532 mL |
| 10 mM | 0.1627 mL | 0.8133 mL | 1.6266 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet