| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Connexin43 hemichannel (Cx43 HC). TAT-Gap19 TFA is a specific inhibitor of Cx43 hemichannels. It binds to the Cx43 protein and blocks the opening or function of the hemichannels, which are implicated in various pathological processes. Importantly, it does not inhibit the gap junction channels that mediate direct cell-cell communication.
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| ln Vitro |
TAT-Gap19 TFA specifically inhibits connexin43 (Cx43) hemichannel activity without affecting Cx43 gap junctional communication. This selectivity makes it an invaluable tool for dissecting the separate functions of hemichannels versus gap junctions. In vitro, it is used to study the role of Cx43 hemichannels in calcium signaling, ATP release, and cell death pathways.
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| ln Vivo |
In 4-month-old C57Bl6 male mice, a single intravenous injection of TAT-Gap19 TFA (iv; 55 mg/kg) results in a notable immunological signal in the brain 24 hours later[1]. Mice treated with 100–200 mg thioacetamide (TAA)/kg body weight for eight weeks[2] showed dramatically reduced collagen deposition and lowed levels of α-SMA-positive cell area when given TAT-Gap19 TFA (1 mg/kg /day) via an osmotic pump implanted in the peritoneal cavity.
In vivo, TAT-Gap19 TFA traverses the blood-brain barrier and has been shown to alleviate liver fibrosis in mice. By inhibiting Cx43 hemichannels, it reduces the release of pro-inflammatory and pro-fibrotic signals, leading to therapeutic effects. This demonstrates the potential of targeting Cx43 hemichannels for treating liver and neurological diseases. |
| Enzyme Assay |
Cx43 hemichannel activity assay (non-cell-based): Liposomes containing purified Cx43 protein are prepared. Dye influx assays with fluorescent dyes (e.g., Lucifer Yellow, 1-5 uM) are performed. Increasing concentrations of TAT-Gap19 TFA (0-1000 nM) are pre-incubated with the proteoliposomes, and the rate of dye uptake is measured by fluorescence. IC50 for hemichannel inhibition is calculated.
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| Cell Assay |
Cx43-expressing cells (e.g., HeLa or astrocytes) are seeded in 12-well plates. Cells are treated with TAT-Gap19 TFA (0.1-100 uM) for 30-60 min. Hemichannel activity is measured by adding a fluorescent tracer (e.g., Lucifer Yellow or ethidium bromide, 1-5 uM) to the culture medium. After 5-15 min, cells are washed and imaged. The number of dye-positive cells is quantified by fluorescence microscopy or flow cytometry.
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| Animal Protocol |
Liver fibrosis model: Male C57BL/6 mice are subjected to bile duct ligation (BDL) or injected with carbon tetrachloride (CCl4) to induce liver fibrosis. TAT-Gap19 TFA is administered intraperitoneally at doses of 5-20 mg/kg, daily or every other day for 2-4 weeks. Liver tissue is collected for histology (Masson's trichrome, Sirius red) and hydroxyproline assay. Markers of fibrosis and inflammation are measured by Western blot and qRT-PCR.
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| ADME/Pharmacokinetics |
As a Tat-conjugated peptide, TAT-Gap19 TFA can cross the blood-brain barrier and is stable in circulation. Pharmacokinetic data are limited but suggest a short plasma half-life (minutes to hours) and distribution to the liver and brain. It is typically administered via intraperitoneal (i.p.) or intravenous (i.v.) injection. The TFA salt enhances solubility.
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| Toxicity/Toxicokinetics |
Toxicity data for TAT-Gap19 TFA are limited to preclinical studies. At therapeutic doses (5-20 mg/kg, i.p.), the compound is generally well-tolerated in mice. As an inhibitor of Cx43 hemichannels, on-target effects may include modulation of physiological processes involving Cx43, such as neuroprotection and inflammation. The compound is intended for research use only.
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| References |
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| Additional Infomation |
TAT-Gap19 TFA is a research-grade peptide inhibitor of Cx43 hemichannels. It has not entered clinical trials or received regulatory approval for human use. It is a valuable tool for studying the role of Cx43 hemichannels in a wide range of diseases, including liver fibrosis, stroke, traumatic brain injury, and retinal degeneration. For research use only.
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| Molecular Formula |
C121H213F3N46O28
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| Molecular Weight |
2817.27
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| Related CAS # |
TAT-Gap19;1507930-54-2
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| Appearance |
White to off-white solid powder
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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, avoid exposure to moisture. |
| 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 :~100 mg/mL (~35.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (35.50 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 | 0.3550 mL | 1.7748 mL | 3.5495 mL | |
| 5 mM | 0.0710 mL | 0.3550 mL | 0.7099 mL | |
| 10 mM | 0.0355 mL | 0.1775 mL | 0.3550 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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