| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
NF-kappaB, MAPK pathways, FPR2 (Formyl Peptide Receptor 2)
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| ln Vitro |
Ac2-26 TFA inhibits the activation of the NF-kappaB and MAPK signaling pathways. It induces the reduction of IKKbeta protein levels in lysosomes through chaperone-mediated autophagy (CMA). In vitro, it suppresses the inflammatory response in various cell types, reducing the production of pro-inflammatory cytokines.
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| ln Vivo |
In vivo, Ac2-26 TFA alleviates ischemia-reperfusion-induced acute lung injury. It also reduces airway inflammation and hyperresponsiveness in asthma model rats. Its anti-inflammatory effects make it a potential therapeutic agent for inflammatory diseases.
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| Enzyme Assay |
In a receptor binding assay, the peptide is dissolved in a suitable buffer. Membrane preparations from cells overexpressing FPR2 are incubated with a labeled agonist (e.g., [125I]-AnxA1) in the presence of varying concentrations of Ac2-26. After a 30-60 minute incubation at room temperature, the mixture is filtered through a glass fiber filter. The retained radioactivity is measured to determine its binding affinity and displacement activity.
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| Cell Assay |
For cell-based assays, RAW264.7 macrophages are seeded in a 6-well plate and cultured to confluence. The cells are pre-incubated with various concentrations of Ac2-26 TFA for 1 hour. Then, an inflammatory stimulus such as LPS (1 ug/mL) is added for 6 hours. Total protein or RNA is extracted. IKKbeta protein levels are measured by Western blot, and pro-inflammatory cytokine (e.g., TNF-alpha, IL-6) mRNA levels are measured by qRT-PCR.
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| Animal Protocol |
In a rat model of asthma, animals are sensitized and challenged with ovalbumin to induce airway inflammation. The test compound, Ac2-26 TFA, is administered via intraperitoneal injection at a specific dose (e.g., 1 mg/kg) daily for 7 days. After the final challenge, bronchoalveolar lavage fluid (BALF) is collected. Total inflammatory cell counts are performed, and cytokine levels (e.g., IL-4, IL-5, IL-13) in the BALF are measured by ELISA. Lung tissues are also collected for histopathological analysis.
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| ADME/Pharmacokinetics |
As a therapeutic peptide, Ac2-26 may have a short plasma half-life due to rapid proteolytic cleavage. Its in vivo stability can be a limiting factor for its clinical application. Pharmacokinetic studies in rodents typically involve IV injection, followed by serial blood collection and analysis of the intact peptide using LC-MS/MS.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data is available for Ac2-26 TFA. Based on its mechanism of inhibiting NF-kappaB, long-term suppression of this pathway could potentially lead to immunosuppression and increased risk of infections. It is used in research to study the molecular mechanisms of inflammation.
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| References | |
| Additional Infomation |
The annexin A1 protein is a known mediator of the anti-inflammatory action of glucocorticoids. Ac2-26 is a research tool to understand how glucocorticoids, such as dexamethasone, exert their potent anti-inflammatory effects. It has potential as a new class of anti-inflammatory drugs but is not yet clinically approved.
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| Molecular Formula |
C143H211F3N32O46S
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|---|---|
| Molecular Weight |
3203.45
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| Related CAS # |
Ac2-26;151988-33-9;Ac2-26 ammonium
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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 (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) |
DMSO :~50 mg/mL (~15.61 mM)
H2O :~1.93 mg/mL (~0.60 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (0.31 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3122 mL | 1.5608 mL | 3.1216 mL | |
| 5 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | |
| 10 mM | 0.0312 mL | 0.1561 mL | 0.3122 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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