Gap 27 (Synonyms: Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile ) |
| Katalog-Nr.GP10119 |
A connexin-mimetic peptide
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 198284-64-9
Sample solution is provided at 25 µL, 10mM.
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.
Referenceㄩ
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).
| Cell experiment: [1] | |
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Cell lines |
Rat osteoclasts |
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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. |
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Reaction Conditions |
500 μM, 48 hours |
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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] | |
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Animal models |
Female Sprague-Dawley rats |
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Dosage form |
300 μM, 45 min |
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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. |
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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. |
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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. | |
| Cas No. | 198284-64-9 | SDF | |
| Überlieferungen | 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 |
| Löslichkeit | ≥65.25mg/mL in DMSO, ≥5mg/mL in Water | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7665 mL | 3.8327 mL | 7.6655 mL |
| 5 mM | 0.1533 mL | 0.7665 mL | 1.5331 mL |
| 10 mM | 0.0767 mL | 0.3833 mL | 0.7665 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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