TAT-Gap19 TFA |
Catalog No.GC62257
One-Click Copy Product Info
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Cx 모방 펩티드인 TAT-Gap19 TFA는 특정 connexin43 반채널(Cx43 HC) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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TAT-Gap19 TFA is a Cx mimetic peptide and a specific inhibitor of connexin 43 (Cx43) hemichannels (HCs)[1-2]. TAT-Gap19 TFA blocks Cx43 hemichannel activity by inhibiting glutamate-induced ATP release, and can cross the blood-brain barrier to reduce cerebral infarct volume and alleviate liver fibrosis. TAT-Gap19 TFA can be used for research related to cerebral ischemia-reperfusion injury and liver fibrosis[3-4].
In vitro, TAT-Gap19 TFA (400µM) treatment of gingival fibroblasts for 24 hours. TAT-Gap19 TFA significantly upregulated the expression of genes including various MMPs, TGF-β signaling molecules, Tenascin-C, and VEGF-A, while significantly downregulating the expression of pro-fibrotic molecules including various extracellular matrix proteins, myofibroblast, and cell contractility-related molecules[5]. Human coronary artery endothelial cells (TICAE) and human microvascular endothelial cells (TIME) were pretreated with TAT-Gap19 TFA (100µM) for 30 minutes, followed by X-ray irradiation (0.1 and 5Gy). TAT-Gap19 TFA significantly reduced radiation-induced intracellular reactive oxygen species (ROS) production, cell death, the expression of pro-inflammatory factors/adhesion molecules, and premature cellular senescence, thereby alleviating radiation-induced endothelial cell damage[6].
In vivo, Balb/c mice with liver fibrosis induced by eight weeks of thioacetamide (TAA) administration were treated with TAT-Gap19 TFA (1mg/kg/day) via an osmotic pump implanted in the peritoneal cavity for two weeks. TAT-Gap19 TFA significantly reduced hepatic collagen deposition and the number of activated hepatic stellate cells (α-SMA-positive cells), increased superoxide dismutase (SOD) activity, and decreased lymphotactin production[7]. C57BL/6 mice with non-alcoholic steatohepatitis (NASH) were treated with TAT-Gap19 TFA (1mg/kg/day, delivered continuously via an implanted osmotic pump for two weeks). TAT-Gap19 TFA significantly reduced liver steatosis score, lobular inflammation score, NAFLD activity score (NAS), hepatic triglyceride and cholesterol levels, and levels of the pro-inflammatory cytokines IL-1β and TNF-α, while increasing SOD activity[8].
References:
[1] Abudara V, Bechberger J, Freitas-Andrade M, et al. The connexin43 mimetic peptide Gap19 inhibits hemichannels without altering gap junctional communication in astrocytes. Front Cell Neurosci. 2014 Oct 21;8:306.
[2] Crespo Yanguas S, da Silva TC, Pereira IVA, et al. TAT-Gap19 and Carbenoxolone Alleviate Liver Fibrosis in Mice. Int J Mol Sci. 2018 Mar 12;19(3):817.
[3] Walrave L, Pierre A, Albertini G, et al. Inhibition of astroglial connexin43 hemichannels with TAT-Gap19 exerts anticonvulsant effects in rodents. Glia. 2018 Aug;66(8):1788-1804.
[4] Quan M, Lv H, Liu Z, et al. MST1 Suppresses Disturbed Flow Induced Atherosclerosis. Circ Res. 2022 Oct 14;131(9):748-764.
[5] Tarzemany R, Jiang G, Jiang JX, et al. Connexin 43 Hemichannels Regulate the Expression of Wound Healing-Associated Genes in Human Gingival Fibroblasts. Sci Rep. 2017 Oct 26;7(1):14157.
[6] Ramadan R, Vromans E, Anang DC, et al. Connexin43 Hemichannel Targeting With TAT-Gap19 Alleviates Radiation-Induced Endothelial Cell Damage. Front Pharmacol. 2020 Mar 5;11:212.
[7] Crespo Yanguas S, da Silva TC, et al. TAT-Gap19 and Carbenoxolone Alleviate Liver Fibrosis in Mice. Int J Mol Sci. 2018 Mar 12;19(3):817.
[8] Willebrords J, Cogliati B, Pereira IVA, et al. Inhibition of connexin hemichannels alleviates non-alcoholic steatohepatitis in mice. Sci Rep. 2017 Aug 15;7(1):8268.
| Cell experiment [1]: | |
Cell lines | TICAE (telomerase-immortalized human coronary artery endothelial cells) and TIME (telomerase-immortalized human microvascular endothelial cells) |
Preparation Method | TICAE and TIME cells were pretreated with 100μM TAT-Gap19 TFA for 30 minutes and then exposed to X-ray irradiation (0.1 and 5Gy). |
Reaction Conditions | 100μM; 30min pretreatment. |
Applications | TAT-Gap19 TFA significantly reduced radiation-induced intracellular reactive oxygen species (ROS) production, cell death (including apoptosis and necrosis), the expression of pro-inflammatory factors/adhesion molecules (including IL-1β, IL-8, VCAM-1, MCP-1, and Endothelin-1), and premature cellular senescence, thereby alleviating radiation-induced endothelial cell damage. |
| Animal experiment [2]: | |
Animal models | Male Balb/c mice |
Preparation Method | Liver fibrosis was induced in mice by intraperitoneal administration of thioacetamide (TAA) for eight weeks. Thereafter, mice were treated with TAT-Gap19 TFA via an osmotic pump implanted in the peritoneal cavity for two weeks. |
Dosage form | 1mg/kg/day; continuous delivery via osmotic pump for two weeks. |
Applications | TAT-Gap19 TFA treatment significantly decreased hepatic collagen deposition and the quantity of activated hepatic stellate cells (α-SMA-positive cells), increased superoxide dismutase (SOD) activity, and reduced the production of the inflammatory protein lymphotactin. |
References: | |
| Cas No. | SDF | ||
| Formula | C121H213F3N46O28 | M.Wt | 2817.27 |
| Solubility | H2O : 100 mg/mL (35.50 mM; Need ultrasonic) | Storage | Store 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 355 μL | 1.7748 mL | 3.5495 mL |
| 5 mM | 71 μL | 355 μL | 709.9 μL |
| 10 mM | 35.5 μL | 177.5 μL | 355 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)