Gap 26
(Synonyms: Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg ) 目录号 : GP10107
Gap 26，作为一种模拟连接蛋白的肽，含有对连接子对接生成间隙连接至关重要的SHVR氨基酸区域。
Cas No.:197250-15-0
Sample solution is provided at 25 µL, 10mM.
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Gap 26, as a connexin mimetic peptide, which has the SHVR amino acid regions contributing crucially to the docking of connexons to generate gap junctions[1]. Gap 26 can inhibit the release of ATP induced by an increase in calcium[2]. Gap 26 inhibited electrical coupling in cell pairs mediated by gap junctions[3].
Gap 26 (25μM; 24h) attenuated the apoptosis of tubular epithelial cells[4]. Gap 26 (150μM; 24h) decreased ROS production, inhibited ASK1-JNK/p38 signaling, and decreased apoptosis in the alveolar type II epithelial cells of rats (RLE-6TN)[5].
Gap 26 (1μg/kg/day; i.p. ; 3 times a week for 8 weeks) alleviated the chronotropic hyporesponsiveness and the severity of liver damage and had an antioxidant effect on the heart in cirrhotic cardiomyopathy rats model[6]. Gap 26 (25μg/kg; i.p. ; 4 day) further deteriorated the destruction of synapses and decreased the spine density of hippocampal in middle cerebral artery occlusion (MCAO) rats model[7].
References:
[1] BOITANO S, EVANS W H. Connexin mimetic peptides reversibly inhibit Ca(2+) signaling through gap junctions in airway cells [J]. American journal of physiology Lung cellular and molecular physiology, 2000, 279(4): L623-30.
[2] BRAET K, VANDAMME W, MARTIN P E, et al. Photoliberating inositol-1,4,5-trisphosphate triggers ATP release that is blocked by the connexin mimetic peptide gap 26 [J]. Cell calcium, 2003, 33(1): 37-48.
[3] DESPLANTEZ T, VERMA V, LEYBAERT L, et al. Gap26, a connexin mimetic peptide, inhibits currents carried by connexin43 hemichannels and gap junction channels [J]. Pharmacol Res, 2012, 65(5): 546-52.
[4] TANG L, YU J, ZHUGE S, et al. Oxidative stress and Cx43-mediated apoptosis are involved in PFOS-induced nephrotoxicity [J]. Toxicology, 2022, 478(153283.
[5] QING C, XINYI Z, XUEFEI Y, et al. The Specific Connexin 43-Inhibiting Peptide Gap26 Improved Alveolar Development of Neonatal Rats With Hyperoxia Exposure [J]. Front Pharmacol, 2021, 12(587267.
[6] MOHAMMED D, TAVANGAR S M, KHODADOOSTAN A, et al. Effects of Gap 26, a Connexin 43 Inhibitor, on Cirrhotic Cardiomyopathy in Rats [J]. Cureus, 2024, 16(4): e59053.
[7] YANG K, ZHOU Y, ZHOU L, et al. Synaptic Plasticity After Focal Cerebral Ischemia Was Attenuated by Gap26 but Enhanced by GAP-134 [J]. Front Neurol, 2020, 11(888.
Gap 26，作为一种模拟连接蛋白的肽，含有对连接子对接生成间隙连接至关重要的SHVR氨基酸区域[1]。Gap 26可以抑制钙升高引起的ATP释放[2]。Gap 26能够抑制由连接蛋白43半通道和间隙连接通道所携带的电流[3]。
Gap 26（25μM；24h）可减少管状上皮细胞的凋亡[4]。Gap 26（150μM; 24h）可降低大鼠肺泡II型上皮细胞（RLE-6TN）的ROS生成，抑制ASK1-JNK/p38信号通路，减少凋亡[5]。
使用Gap 26（1μg/kg/day; i.p. ; 3 times a week for 8 weeks）处理肝硬化心肌病模型大鼠，Gap26可减轻大鼠的变时性反应低下和肝损害程度，并对心脏具有抗氧化作用[6]。使用Gap 26（25μg/kg; i.p. ; 4 day）处理MCAO（middle cerebral artery occlusion，大脑中动脉闭塞）模型大鼠，Gap 26进一步加重了大鼠脑中的突触破坏，降低了大鼠脑中海马棘密度[7]。
| Cell experiment [1]: | |
Cell lines | Normal rat kidney epithelial (NRK52E) cell |
Preparation Method | NRK52E cells were cultured in Dulbecco’s Modified Eagle’s Medium supplemented with 10% fetal bovine serum. NRK52E cells were exposed to Gap 26 for 24h. |
Reaction Conditions | 25μM; 24h |
Applications | Gap 26 (25μM; 24h) attenuated the apoptosis of tubular epithelial cells. |
| Animal experiment [2]: | |
Animal models | Male CD1 mice |
Preparation Method | Rats were anesthetized with 10% chloral hydrate. Subsequently, a mid-line incision was made in the neck of rats. The right common carotid artery (CCA), external carotid artery (ECA), and internal carotid artery (ICA) were isolated. The ECA was cut approximately 4mm above the common carotid artery bifurcation. A 4.0-s nylon monofilament suture was inserted into ICA through the stump until resistance. In this way, the blood flow to the middle cerebral artery (MCA) was blocked. 2h later, the filament was taken out for reperfusion, and the incision was ligated. Gap 26 was dissolved in saline and given intraperitoneally at the dose of 25μg/kg once a day. To avoid the influence in the acute phase, we chose to apply Gap 26 from day 3 after ischemia, when the infarction volume stabilized and the repair period began. At 7 day after MCAO, rats were sacrificed, and brains were removed as soon as possible. Rapid Golgi Stain Kit was applied for tissue preparation and staining procedures. The whole Golgi-Cox staining procedures were conducted in strict accordance with instructions. Using a freezing microtome, each block was then cut coronally into 100-μm-thick serial sections starting at +1.00 to 5.00mm from the bregma. The sections were mounted onto slides and observed under a laser scanning confocal microscope. |
Dosage form | 25μg/kg; 4 day; i.p. |
Applications | Gap 26 further deteriorated the destruction of synapses and decreased the spine density of hippocampal in middle cerebral artery occlusion (MCAO) rats model. |
References: | |
| Cas No. | 197250-15-0 | SDF | |
| 别名 | Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg | ||
| 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 Water with ultrasonic | 储存条件 | -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.6448 mL | 3.2242 mL | 6.4483 mL |
| 5 mM | 0.129 mL | 0.6448 mL | 1.2897 mL |
| 10 mM | 0.0645 mL | 0.3224 mL | 0.6448 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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