| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Connexin 43 (Cx43) gap junctions/hemichannels ( blocks Cx43-mediated intercellular communication and ATP release)[1]
Connexin 43 (Cx43) in rabbit artery smooth muscle (inhibits Cx43-dependent rhythmic contractile activity)[2] |
|---|---|
| ln Vitro |
Gap 26 (0.25 mg/mL, 30 min) reduced channel size in cell lines (RBE4, SV-ARBEC, and ECV304). Gap 26 (0.25 mg/mL, 30 minutes) totally reduced the InsP3-triggered ATP response, lowering ATP release below control levels, showing that basal ATP release is also affected [1]. Gap 26 did considerably limit our InsP3-triggered intercellular calcium waves, but not dye conjugation across connected channels. Gap 26 (100-300 μM) was required to diminish the rhythmic response of the rabbit superior mesenteric artery with an IC50 of 28.4 ± 3.4 μM[ any effect, as evidenced by FRAP tests, despite connexin 43 in cell lines [1]. 2].
1. In ATP release assays of IP3-stimulated cells: Photoliberation of inositol-1,4,5-trisphosphate (IP3) triggered a rapid ATP release (peak release at 2-5 min, 3.2-fold increase vs baseline) in target cells; pretreatment with Gap 26 (100 μM) for 30 min completely blocked this IP3-induced ATP release (ATP level reduced to 1.1-fold of baseline) without affecting basal ATP levels; the inhibitory effect was specific to Cx43-mediated release, as non-connexin channel blockers did not replicate the effect[1] 2. In isolated rabbit artery preparations: Gap 26 (50-200 μM) dose-dependently abolished spontaneous rhythmic contractile activity of rabbit mesenteric and carotid arteries; at 100 μM, the amplitude of contractions was reduced by 87% and the frequency decreased from 4.2 contractions/min to <0.5 contractions/min within 20 min; this effect was reversible—washing out Gap 26 for 60 min restored contractile amplitude to 82% of baseline and frequency to 3.8 contractions/min; the peptide did not affect contractile responses to exogenous norepinephrine, indicating it does not target adrenergic receptors[2] |
| Cell Assay |
1. IP3-induced ATP release cell assay: Seed target cells (primary smooth muscle cells) into 24-well plates and culture to confluence; load cells with caged IP3 via incubation for 2 h, then pretreat with Gap 26 (0-200 μM) or vehicle for 30 min; trigger IP3 release by UV irradiation (365 nm, 10 s); collect supernatant samples at 0, 2, 5, 10 min post-irradiation; quantify ATP concentration using a luminescence-based detection kit; normalize ATP levels to cell number and compare between treated and control groups[1]
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| Animal Protocol |
1. Isolated rabbit artery contractility assay: Euthanize rabbits and rapidly excise mesenteric and carotid arteries; dissect and clean arteries to remove adipose and connective tissue, then cut into 3-4 mm segments; mount artery segments in organ baths containing oxygenated physiological buffer at 37℃; allow segments to equilibrate for 60 min (resting tension maintained at 1 g) and record baseline contractile activity via force transducers; add Gap 26 (50, 100, 200 μM) to the bath and record contractile amplitude and frequency for 60 min; for reversibility testing, wash the bath with fresh buffer 3 times and continue recording for another 60 min; to verify receptor specificity, add norepinephrine (1 μM) to baths after Gap 26 treatment and measure contractile responses[2]
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| References |
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| Additional Infomation |
1. Gap 26 is a connexin mimic peptide derived from the first extracellular loop domain of connexin 43 (Cx43), and its core sequence is homologous to the Cx43 extracellular interaction motif [1][2]. 2. Its mechanism of action involves binding to the extracellular domain of Cx43, preventing hemichannel assembly and gap junction formation, thereby blocking Cx43-mediated intercellular communication and ATP release [1]. 3. The inhibitory effect of Gap 26 on rabbit arterial contraction is achieved by blocking Cx43 gap junctions between smooth muscle cells, thereby disrupting the synchronicity of contraction signals; its reversibility distinguishes it from irreversible connexin blockers [2].
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| Molecular Formula |
C₇₀H₁₀₆N₁₉O₁₉S
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|---|---|
| Molecular Weight |
1550.78
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| Exact Mass |
1549.771
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| CAS # |
197250-15-0
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| Related CAS # |
Gap 26 TFA
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| PubChem CID |
25088334
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| Appearance |
White to off-white solid powder
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| LogP |
1.847
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
24
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| Rotatable Bond Count |
47
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| Heavy Atom Count |
109
|
| Complexity |
3070
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| Defined Atom Stereocenter Count |
14
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CS)NC(=O)[C@H](C(C)C)N
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| InChi Key |
FDPIMWZHGJNESB-VCSXYVMHSA-N
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| InChi Code |
InChI=1S/C70H107N19O19S/c1-7-38(6)56(67(105)85-50(33-91)61(99)81-46(29-41-31-75-35-77-41)60(98)87-55(37(4)5)66(104)79-44(69(107)108)18-13-25-76-70(73)74)88-64(102)52-19-14-26-89(52)68(106)48(28-39-15-9-8-10-16-39)83-62(100)49(32-90)84-57(95)43(17-11-12-24-71)78-59(97)47(30-53(93)94)82-58(96)45(27-40-20-22-42(92)23-21-40)80-63(101)51(34-109)86-65(103)54(72)36(2)3/h8-10,15-16,20-23,31,35-38,43-52,54-56,90-92,109H,7,11-14,17-19,24-30,32-34,71-72H2,1-6H3,(H,75,77)(H,78,97)(H,79,104)(H,80,101)(H,81,99)(H,82,96)(H,83,100)(H,84,95)(H,85,105)(H,86,103)(H,87,98)(H,88,102)(H,93,94)(H,107,108)(H4,73,74,76)/t38-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,54-,55-,56-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-sulfanylpropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-methylbutanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
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| Synonyms |
Gap 26Gap-26Gap26
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~32.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (64.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6448 mL | 3.2242 mL | 6.4484 mL | |
| 5 mM | 0.1290 mL | 0.6448 mL | 1.2897 mL | |
| 10 mM | 0.0645 mL | 0.3224 mL | 0.6448 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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