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Gap 27Selective gap junction blocker

Gap 27

Catalog No. A1045
Size Price Stock Qty
5mg $135.00 In stock
10mg $225.00 In stock
25mg $315.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Koenen, Anna, et al. "Effects of renal denervation on renal pelvic contractions and connexin expression in rats." Acta Physiologica (2015). PMID:26436542

Quality Control

Quality Control & MSDS

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Chemical structure

Gap 27

Related Biological Data

Gap 27

Related Biological Data

Gap 27

Biological Activity

Description 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.
Targets            
IC50            

Protocol

Cell experiment: [1]

Cell lines

Rat osteoclasts

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

500 μM, 48 hours

Applications

Heptanol-treated cells acted as positive controls for gap-junctional inhibition. A significant decrease could be seen in the number of both TRAP-positive mononuclear and multinucleated cells with Gap 27 compared to controls. The numbers of TRAP-positive mononuclear and multinucleated cells with both treatments were very similar. After the 48-hour incubation, survival of osteoclasts was clearly reduced in the groups where gap-junctional communication was blocked either by heptanol or Gap 27.

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-27 was initiated. Forty-five minutes later, the neural activation was repeated. Application of gap-27 peptide attenuated bicuculline-induced pial arteriolar dilation (by ~ 50%), without altering neuronal activation. A similar result was obtained with the SNS-associated pial arteriolar response, although the degree of reduction in the vasodilating response (~ 75%) was somewhat greater.

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] 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.

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Chemical Properties

Cas No. 198284-64-9 SDF Download SDF
Synonyms Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile
Chemical Name Gap 27
Canonical SMILES CCC(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
Formula C60H101N15O17 M.Wt 1304.55
Solubility >65.3mg/mL in DMSO Storage Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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).