| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Connexin 43 hemichannel (Cx43 HC). TAT-Gap19 selectively blocks Cx43 hemichannels with an IC50 of approximately 7 μM but does not inhibit Cx43 gap junction channels (GJCs) or Pannexin-1 channels. The compound targets the C-terminal domain of Cx43, interfering with hemichannel opening without affecting intercellular gap junction communication. This selectivity is critical for dissecting hemichannel-specific functions in physiological and pathological contexts.
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| ln Vitro |
TAT-Gap19 inhibits Cx43 hemichannel activity in astrocytes with an IC50 of 7 μM. In vitro studies demonstrate that the peptide does not affect gap junctional communication, distinguishing it from broad-spectrum gap junction blockers. The compound has been shown to reduce hemichannel-mediated ATP release and dye uptake in cell-based assays. These properties make TAT-Gap19 a valuable tool for studying Cx43 hemichannel pathophysiology in neurological and cardiovascular research.
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| ln Vivo |
In 4 month old male C57Bl6 mice, a single intravenous injection of TAT-Gap19 (55 mg/kg) causes a substantial immunological signal in the brain 24 hours later[1]. Mice treated with 100-200 mg thioacetamide (TAA)/kg body weight for eight weeks demonstrate considerably reduced collagen deposition and lowed quantities of α-SMA-positive cell area with TAT-Gap19 (1 mg/kg/day), an osmotic pump implanted in the peritoneal cavity[2].
TAT-Gap19 crosses the blood-brain barrier and exerts anticonvulsant effects in rodent seizure models. In a mouse model of liver fibrosis induced by thioacetamide, intraperitoneal administration of TAT-Gap19 (1 mg/kg/day for two weeks via osmotic pump) significantly decreased collagen deposition and reduced alpha-SMA-positive cell areas. A single intravenous injection (55 mg/kg via tail vein) produced significant brain accumulation within 24 hours in C57Bl/6 mice. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays typically involve measuring hemichannel activity using dye uptake or ATP release assays in cells overexpressing Cx43. The IC50 determination is performed by pre-incubating cells with varying concentrations of TAT-Gap19 (typically 0.1–100 μM) followed by addition of fluorescent dyes such as Lucifer Yellow or ethidium bromide. Hemichannel opening is triggered by removal of extracellular calcium or by metabolic inhibition. Fluorescence intensity is measured over time, and inhibition curves are fitted to calculate IC50 values.
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| Cell Assay |
Cells (e.g., primary astrocytes or Cx43-transfected HeLa cells) are cultured in appropriate media and treated with TAT-Gap19 at concentrations ranging from 1–100 μM for 30 minutes to 4 hours. Hemichannel activity is assessed by dye uptake assay: cells are incubated with Lucifer Yellow (1–5 mM) or ethidium bromide (10–50 μM) in low-calcium buffer to induce hemichannel opening. Fluorescence is quantified by microscopy or plate reader. Gap junction communication is assessed separately by scrape-loading or dye transfer assays to confirm selectivity.
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| Animal Protocol |
In vivo animal studies have been conducted in C57Bl/6 mice. For liver fibrosis models, mice are treated with thioacetamide (100–200 mg/kg) for eight weeks, then TAT-Gap19 is administered via intraperitoneally implanted osmotic pumps at 1 mg/kg/day for two weeks. Fibrosis is evaluated by collagen staining and alpha-SMA immunohistochemistry. For brain distribution studies, a single intravenous injection of 55 mg/kg TAT-Gap19 is given via tail vein, and brain tissue is collected 24 hours post-injection for analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TAT-Gap19 are limited to brain distribution studies showing that the peptide crosses the blood-brain barrier. The TAT cell-penetrating sequence facilitates cellular uptake and tissue penetration. The peptide is typically administered via intravenous or intraperitoneal routes. Systemic half-life and bioavailability have not been fully characterized in peer-reviewed literature. As a peptide, it is expected to be susceptible to proteolytic degradation, requiring formulation strategies for in vivo stability.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for TAT-Gap19 have not been published. The compound is for research use only and not approved for human therapeutic applications. In animal studies at the doses tested (1–55 mg/kg), no acute toxicity was reported; however, systematic toxicological evaluation has not been performed. Standard safety precautions for peptide handling should be observed.
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| References |
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| Additional Infomation |
TAT-Gap19 is a research tool for studying connexin 43 hemichannel biology. It is not in clinical trials and has no regulatory approval for human use. The peptide is supplied as a lyophilized powder and is soluble in water (50 mg/mL). References include studies on hemichannel inhibition in astrocytes, anticonvulsant effects, and liver fibrosis.
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| Molecular Formula |
C119H212N46O26
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|---|---|
| Molecular Weight |
2703.25
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| Exact Mass |
2702.671
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| CAS # |
1507930-54-2
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| Related CAS # |
TAT-Gap19 TFA
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| PubChem CID |
127021051
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| Appearance |
White to off-white solid powder
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| Density |
1.46±0.1 g/cm3(Predicted)
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| LogP |
-14.2
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| Hydrogen Bond Donor Count |
49
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| Hydrogen Bond Acceptor Count |
39
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| Rotatable Bond Count |
110
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| Heavy Atom Count |
191
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| Complexity |
5700
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| Defined Atom Stereocenter Count |
21
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC2=CC=C(C=C2)O)N
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| InChi Key |
ALNCFPIRTLVJPY-LJFAJSDSSA-N
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| InChi Code |
InChI=1S/C119H212N46O26/c1-5-67(3)93(111(188)160-78(34-14-20-56-124)100(177)152-77(33-13-19-55-123)106(183)163-88(65-69-28-8-7-9-29-69)110(187)162-87(113(190)191)35-15-21-57-125)165-109(186)86(48-51-92(170)171)161-112(189)94(68(4)6-2)164-108(185)85(47-50-90(128)168)159-99(176)76(32-12-18-54-122)151-101(178)79(37-23-59-142-115(131)132)154-103(180)81(39-25-61-144-117(135)136)155-104(181)82(40-26-62-145-118(137)138)157-107(184)84(46-49-89(127)167)158-105(182)83(41-27-63-146-119(139)140)156-102(179)80(38-24-60-143-116(133)134)153-98(175)75(31-11-17-53-121)150-97(174)74(30-10-16-52-120)149-96(173)73(36-22-58-141-114(129)130)148-91(169)66-147-95(172)72(126)64-70-42-44-71(166)45-43-70/h7-9,28-29,42-45,67-68,72-88,93-94,166H,5-6,10-27,30-41,46-66,120-126H2,1-4H3,(H2,127,167)(H2,128,168)(H,147,172)(H,148,169)(H,149,173)(H,150,174)(H,151,178)(H,152,177)(H,153,175)(H,154,180)(H,155,181)(H,156,179)(H,157,184)(H,158,182)(H,159,176)(H,160,188)(H,161,189)(H,162,187)(H,163,183)(H,164,185)(H,165,186)(H,170,171)(H,190,191)(H4,129,130,141)(H4,131,132,142)(H4,133,134,143)(H4,135,136,144)(H4,137,138,145)(H4,139,140,146)/t67-,68-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,93-,94-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-phenylpropanoyl]amino]hexanoic acid
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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 : 50 mg/mL (18.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (36.99 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 | 0.3699 mL | 1.8496 mL | 3.6993 mL | |
| 5 mM | 0.0740 mL | 0.3699 mL | 0.7399 mL | |
| 10 mM | 0.0370 mL | 0.1850 mL | 0.3699 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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