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Gap 26

目录号 GP10107

Gap junction blocker peptide, mapping to connexin 43 residue 63-75

规格 价格 库存 购买数量
5mg
¥1,040.00
现货
10mg
¥1,544.00
现货
25mg
¥2,163.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment: [1]

Cell lines

ECV304 cells

Preparation method

The solubility of this peptide in sterile water is >10 mM. Stock solution should be splited and stored at -80°C for several months.

Reaction Conditions

0.25mg/ml, 30min

Applications

Preventing the InsP3-triggered calcium increase by ester loading the cells with the calcium chelator BAPTA reduced the InsP3-triggered ATP release back to the control level. Incubation of the cells with gap 26 completely abolished the InsP3-triggered ATP response and reduced the ATP release to below the control level, indicating that the basal ATP release is also affected.

Animal experiment: [2]

Animal models

Female Sprague-Dawley rats

Dosage form

300 μM, 45 min

Applications

The rats were prepared with closed cranial windows 24 h before the study. A 10-mm-diameter craniotomy was performed over the skull midline. The dura was removed carefully to keep the sagittal sinus intact. An 11-mm-diameter glass window outfitted with three ports was glued to the skull using cyanoacrylate. The skin overlying the window was sutured, and the animals were permitted to recover. On the day of study, three stainless steel screws were inserted into the skull, along the periphery of the cranial window, for electroencephalogram (EEG) recording. Cannulae were then connected to the three ports. The rats were subjected to one of two neuronal activation paradigms: SNS or bicuculline-induced seizure. Following the initial measurement of pial arteriolar diameter changes during SNS or during bicuculline exposure, baseline conditions were reestablished. After 20 min, a suffusion of gap-26 was initiated. Forty-five minutes later, the neural activation was repeated. Exposure to the Cx40/Cx37 inhibitory peptide, gap-26 (300 μM), was without effect on bicuculline- or SNS-induced pial arteriolar dilations.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Braet K, Vandamme W, Martin P E M, et al. Photoliberating inositol-1, 4, 5-trisphosphate triggers ATP release that is blocked by the connexin mimetic peptide gap 26. Cell calcium, 2003, 33(1): 37-48.

[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.

产品描述

Gap26 (Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg) is a connexin mimetic peptide, corresponding to residues 63-75 of connexin 43, which is a 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 molecules. Calcium and inositol phosphates are among the second messengers that can pass through gap junction channels. [1] It was showed that gap26 attenuates rhythmic contractile activity of rabbit arterial smooth muscle (IC50 = 28.4 mM). It also blocks movement of IP3-induced ATP and Ca2+ across connexin hemichannels, i.e. hexameric channels yet to dock with partners in aligned cells and to generate the gap junction cell–cell conduit. [2]

References:
1. Boitano, S. and H. Evans Am. J. Physiol. Lung Cell Mol. Physiol. 279, L623 (2000).
2. T. Desplantez, V. Verma, L. Leybaert, W.H. Evans, R. Weingart, Gap26, a connexin mimetic peptide, inhibits currents carried by connexin43 hemichannels and gap junction channels, Pharmacological Research, Volume 65, Issue 5, May 2012, Pages 546-552.

Chemical Properties

Cas No. 197250-15-0 SDF
别名 Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg
化学名 N/A
Canonical SMILES N/A
分子式 C70H107N19O19S 分子量 1550.79
溶解度 ≥ 77.55 mg/mL in DMSO with ultrasonic and warming, <7.75 mg/mL in EtOH, ≥ 155.1 mg/mL in H2O with ultrasonic 储存条件 -20°C, protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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