GlpBio

SLIGRL-NH2

目录号: GC17514纯度: >99.50%同义词: Protease-Activated Receptor-2 Activating Peptide
SLIGRL-NH2是一种特异性蛋白酶激活受体2（PAR2）激动剂，EC50 值约为10μM，SLIGRL-NH2不会激活PAR1。
SLIGRL-NH2
Cas No.: 171436-38-7
规格价格库存数量操作
1mg¥560.00现货
1
5mg¥1,520.00现货
1
10mg¥2,400.00现货
1
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产品描述 Description

SLIGRL-NH2 is a specific protease-activated receptor 2 (PAR2) agonist with an EC50 value of approximately 10μM. SLIGRL-NH2 does not activate PAR1[1, 2]. SLIGRL-NH2 is a recombinant peptide involved in the regulation of inflammatory responses and pain signaling pathways[3]. The addition of SLIGRL-NH2 to the culture medium can reduce the average neurite length of PC12 neuronal cells[4].

In vivo, SLIGRL-NH2 (2.5μmol/kg, 5μmol/kg) administered orally for 7 days to constipated rats improved their feeding and excretion behaviors, significantly increased the expression of PAR2 in colonic tissue, augmented the number of interstitial Cajal cells, reduced the expression of inhibitory neurotransmitter VIP, and enhanced the expression of excitatory neurotransmitter SP[5]. SLIGRL-NH2 (1mM, 100µL) administered subcutaneously to mice significantly induced hyperalgesia in the mice[6].

References:
[1] Devlin, Mark G., et al. Hepta and octapeptide agonists of protease‐activated receptor 2. Journal of Peptide Science: An Official Publication of the European Peptide Society 13.12 (2007): 856-861.
[2] Boitano, Scott, et al. Development and evaluation of small peptidomimetic ligands to protease-activated receptor-2 (PAR2) through the use of lipid tethering. PloS one 9.6 (2014): e99140.
[3] Van der Merwe, Jacques. Proteinase-activated receptor-2 induces chloride secretion through multiple signaling pathways.(2008).
[4] Nguyen, Cathy. The Promotion of Peripheral Nerve Regeneration by PAR2 Activation Following Induction of Acute Nerve Injury. Library and Archives Canada= Bibliothq̈ue et Archives Canada, 2007.
[5] Zhang, Yonggang, et al. Therapeutic effect of protease-activated receptor 2 agonist SLIGRL-NH2 on loperamide-induced Sprague-Dawley rat constipation model and the related mechanism. Drug Design, Development and Therapy (2018): 2403-2411.
[6] Kido, Kanta, et al. Nociceptive sensitization by activation of protease-activated receptor 2 in a rat model of incisional pain. Brain Sciences 11.2 (2021): 144.

SLIGRL-NH2是一种特异性蛋白酶激活受体2（PAR2）激动剂，EC50 值约为10μM，SLIGRL-NH2不会激活PAR1[1, 2]。SLIGRL-NH2是一种重组肽，参与炎症反应及疼痛信号通路的调控[3]。SLIGRL-NH2补充到培养基里能够减少 PC12神经元细胞的平均神经突长度[4]。

在体内，SLIGRL-NH2（2.5μmol/kg, 5μmol/kg）通过口服治疗便秘大鼠7天，改善了便秘大鼠的进食和排泄行为，显著增加了结肠组织的PAR2表达，并增加间质Cajal细胞数量，降低了抑制性神经递质VIP的表达，提高了兴奋性神经递质SP的表达[5]。SLIGRL-NH2（1mM, 100µL）通过皮下注射处理小鼠，显著诱发了小鼠的痛觉过敏[6]。

实验参考方法 Experimental Reference Method

Animal experiment [1]:

Animal models

Sprague-Dawley (SD) rat

Preparation Method

Loperamide was injected subcutaneously to induce constipation twice a day for 3 days. SD rats were randomly divided into five groups: non-constipation group, constipation group, constipation+SLIGRL-NH2 low-dosage group, constipation+SLIGRL-NH2 high-dosage group, and constipation+prucalopride. The SLIGRL-NH2 low group and SLIGRL-NH2 high group were administered with 2.5μmol/kg and 5μmol/kg SLIGRL-NH2, respectively, and the prucalopride group received 2mg/kg prucalopride. The control and constipation group received 1× PBS under the same pattern. SLIGRL-NH2 and prucalopride were orally administrated once daily for 7 days. On the final day of oral administration, food intake, water intake, the number of stool pellets, weight, and fecal water content was calculated; moreover, the colons of rats in different groups were collected and histological features were examined by hematoxylin and eosin staining; furthermore, the expression of anoctamin-1 was determined by Immunohistochemical methods, and the expressions of c-kit and PAR-2 were examined using real-time quantitative polymerase chain reaction and Western blot methods; finally, the expressions of neurotransmitter vasoactive intestinal peptide (VIP) and substance P (SP) were examined using enzyme-linked immuno-sorbent assay methods.

Dosage form

2.5μmol/kg, 5μmol/kg; 7 days; p.o.

Applications

The feeding and excretion behaviors, intestinal transit ratio, and the histological feature of the colon in the constipated rats were all improved by SLIGRL-NH2 treatment; moreover, SLIGRL-NH2 treatment induced significant increase in the expression of PAR-2 and also increased number of interstitial Cajal cells. Furthermore, SLIGRL-NH2 also decreased the contents of the inhibitory neurotransmitter VIP and increased the expression of the excitatory neurotransmitter SP. High dose of SLIGRL-NH2 has shown similar anti-constipation effects as prucalopride.

References:
[1] Zhang, Yonggang, et al. Therapeutic effect of protease-activated receptor 2 agonist SLIGRL-NH2 on loperamide-induced Sprague-Dawley rat constipation model and the related mechanism. Drug Design, Development and Therapy (2018): 2403-2411.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
171436-38-7
同义词
Protease-Activated Receptor-2 Activating Peptide
化学名
(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-N-[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]-3-methylpentanamide
SMILES
CCC(C)C(C(=O)NCC(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CO)N
分子式
C29H56N10O7
分子量
656.82 g/mol
溶解性
H<sub>2</sub>O : 110 mg/mL (167.47 mM; Need ultrasonic); DMSO : 100 mg/mL (152.25 mM; Need ultrasonic)
保存条件
Desiccate at -20&deg;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°C，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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol