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Gap 27

现货
Catalog No.
A1045
缝隙连接阻断剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,350.00
现货
10mg
¥ 2,250.00
现货
25mg
¥ 3,150.00
现货

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Background

Gap 27 is a peptide(Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile) derived from connexin 43 that is a selective gap junction blocker.

Connexins, or gap junctions, are a family of structurally-related transmembrane proteins. Gap junctions contain channels that allow the passage of ions and small molecules between adjacent cells. This intercellular communication has been implicated in the coordination of cellular responses to intracellular signaling molecules. Calcium and inositol phosphates are among the second messengers that can pass through gap junction channels. This synthetic connexin-mimetic peptide, Gap 27, was used to evaluate the contribution of gap-junctional communication to osteoclastic bone resorption. It was concluded that gap-junctional communication is necessary for proper bone remodeling.

A1045_1 

Figure1  Formula of Gap 27

Ref:

1. Berthoud, V. et al. Am. J. Physiol. Lung Cell Mol. Physiol. 279, 619 (2000)

2. Ilvesaro, J. et al. BMC Musculoskel. Disord. 2, 10 (2001)

3. Chaytor, A. et al. Brit. J. Pharmacol. 144, 108 (2005)

4. Boitano, S. and H. Evans Am. J. Physio.l Lung Cell Mol. Physiol. 279, L623 ( 2000).

文献引用

1.Ni X, Li XZ, et al. "Increased expression and functionality of the gap junction in peripheral blood lymphocytes is associated with hypertension-mediated inflammation in spontaneously hypertensive rats." Cell Mol Biol Lett. 2018 Aug 20;23:40. PMID:30151015
2.HAI-CHAO ZHANG, ZHONG-SHUANG ZHANG, et al."Connexin 43 in splenic lymphocytes is involved in the regulation of CD4+ CD25+ T lymphocyte proliferation and cytokine production in hypertensive inflammation." INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE. 2017 October 20.
3.Ni X, Wang A, et al. "Up-regulation of gap junction in peripheral blood T lymphocytes contributes to the inflammatory response in essential hypertension." PLoS One. 2017 Sep 14;12(9):e0184773. PMID:28910394
4.Koenen, Anna, et al. "Effects of renal denervation on renal pelvic contractions and connexin expression in rats." Acta Physiologica (2015). PMID:26436542

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt1304.55
Cas No.198284-64-9
FormulaC60H101N15O17
SynonymsSer-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile
Solubility≥65.25mg/mL in DMSO, ≥5mg/mL in H2O
Chemical NameGap 27
SDFDownload SDF
Canonical SMILESCCC(C)C(C(=O)NC(C(C)CC)C(=O)O)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(C(C)CC)NC(=O)C(C(C)O)NC(=O)C(CCCCN)NC(=O)C(CCC(=O)O)NC(=O)C(C(C)O)NC(=O)C2CCCN2C(=O)C(CCCN=C(N)N)NC(=O)C(CO)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

大鼠破骨细胞

溶解方法

Gap 27在无菌水中的溶解度大于10 mM,分装储存于-80℃,可储存数月。

反应时间

500 μM, 48 小时

实验结果

实验中,将使用庚醇处理的细胞作为缝隙连接抑制的阳性对照组。与对照相比,使用Gap27处理的TRAP阳性单核和多核细胞的数量显著减少。庚醇或Gap27处理的TRAP阳性单核和多核细胞的数量非常相似。庚醇或Gap27孵育48小时后,阻断缝隙连接,破骨细胞的存活率明显降低。

动物实验[2] :

动物模型

雌性Sprague-Dawley大鼠

剂量

300 μM, 45 min

实验结果

在进行研究之前24小时,制备具有封闭颅窗的大鼠模型。在头骨中线上进行直径10 mm的开颅手术,小心地移除硬膜以保持矢状窦完整。使用氰基丙烯酸酯将装备有三个端口的11 mm直径的玻璃窗粘合到颅骨,缝合窗口的皮肤使动物康复。在研究当天,将三个不锈钢螺钉沿颅窗的周边插入颅骨,用于脑电图(EEG)记录。然后将套管连接到三个端口。使大鼠经受两种神经元活化的其中一种:SNS或bicuculline诱导的癫痫发作。在SNS或Bicuculline给药期间对小动脉直径的变化进行初始测量,重建基线条件。20分钟后加入gap-27。45分钟后,神经重新激活。Gap-27将bicuculline诱导的软膜小动脉扩张减弱了约50%,但未改变神经元活化。SNS相关的软膜小动脉应答获得了类似的结果,但血管扩张反应的减少程度较大,约为75%。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Ilvesaro J, Tavi P, Tuukkanen J. Connexin-mimetic peptide Gap 27 decreases osteoclastic activity. BMC musculoskeletal disorders, 2001, 2(1): 10.

[2] Xu H L, Mao L, Ye S, et al. Astrocytes are a key conduit for upstream signaling of vasodilation during cerebral cortical neuronal activation in vivo. American Journal of Physiology-Heart and Circulatory Physiology, 2008, 294(2): H622-H632.

生物活性

Description Gap 27是来源于connexin 43的多肽(Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile),是缝隙连接的选择性阻断剂。
Targets            
IC50            

质量控制

化学结构

Gap 27

相关生物数据

Gap 27

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Gap 27

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Gap 27

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Gap 27

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Gap 27