| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Ac2-26 ammonium targets two key formyl peptide receptors (FPRs): FPR1 and FPR2/ALX (also known as FPRL1), with EC50 values of 1.4 μM and 1.8 μM, respectively. These receptors are part of the GPCR family and are expressed on various immune cells, including neutrophils, monocytes, and macrophages. The engagement of FPR2/ALX by Ac2-26 is particularly important for its anti-inflammatory actions, as this receptor is a well-known mediator of pro-resolving signals. By activating these receptors, Ac2-26 initiates downstream signaling cascades that modulate cell migration, cytokine production, and other inflammatory responses. Additionally, Ac2-26 ammonium has been shown to induce a decrease in IKKβ protein in lysosomes via chaperone-mediated autophagy (CMA), thereby modulating NF-κB signaling and further contributing to its anti-inflammatory effects.
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| ln Vitro |
In radioligand binding assays, Ac2-26 ammonium demonstrates the ability to bind to HEK293 cells expressing human FPR1 or FPR2. Functionally, Ac2-26 (10 and 100 µg/ml) inhibits lipopolysaccharide (LPS)-induced production of prostaglandin E2 and nitric oxide (NO) in rat microglial cells. In human THP-1 monocyte cells, it significantly activates the expression of heme oxygenase-1 (HO-1), an anti-inflammatory gene downstream of Nrf2. Furthermore, in LPS-induced HK-2 cells, Ac2-26 ammonium at 0.5 μM for 24 hours inhibits the production of inflammatory cytokines and apoptosis. Ac2-26 is also a genuine chemokinetic agent, capable of inducing the migration of human neutrophils and monocytes. This chemokinetic activity is mediated by both FPR1 and FPR2, and primarily involves the ERK, but not JNK and p38, MAPK signaling pathways.
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| ln Vivo |
In vivo, Ac2-26 ammonium has demonstrated significant anti-inflammatory and protective effects across multiple animal models. In a rat model of ventilator-induced ischemia-reperfusion injury, administration of Ac2-26 at doses of 0.5 and 1 mg/kg effectively reduces pulmonary edema. It also alleviates liver ischemia-reperfusion injury in mice by regulating the IL-22/IL-22R1/STAT3 signaling pathway and eNOS pathways. In a mouse model of pneumococcal meningitis, Ac2-26 mediates an anti-inflammatory response via FPR2 expressed by brain immune cells. Additionally, it inhibits airway inflammation and hyperresponsiveness in an asthma rat model, and shows efficacy in a mouse model of neuroinflammation. The peptide's ability to regulate both insulin secretion and glucose production further suggests a role in metabolic regulation.
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| Enzyme Assay |
Non-cellular receptor binding assays for Ac2-26 ammonium are typically performed using radioligand binding techniques with HEK293 cells that have been engineered to express human FPR1 or FPR2. In these assays, the compound is incubated with the cells and a labeled ligand that competes for the same binding site. The binding affinity is then determined by measuring the displacement of the radioligand, and EC50 values are calculated from dose-response curves. To study the direct interaction between Ac2-26 and its receptors, surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be employed using recombinant receptor proteins, providing detailed kinetic and thermodynamic data on the binding event.
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| Cell Assay |
In vitro cellular assays are central to characterizing the bioactivity of Ac2-26 ammonium. These assays typically involve treating various cell types, such as rat microglia, human THP-1 monocytes, or HK-2 kidney cells, with the peptide. In LPS-stimulated microglia, the inhibition of prostaglandin E2 and NO production is measured to assess its anti-inflammatory effect. For THP-1 cells, the activation of the Nrf2 pathway and the subsequent increase in HO-1 expression are evaluated via qRT-PCR and Western blotting. In HK-2 cells, the peptide's protective effect against LPS-induced apoptosis and cytokine production is quantified. The chemokinetic activity of Ac2-26 is assessed using chemotaxis chambers, where the migration of primary human neutrophils or monocytes towards a gradient of the peptide is measured.
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| Animal Protocol |
In vivo animal experiments are crucial for validating the therapeutic potential of Ac2-26 ammonium. The peptide is typically administered via intraperitoneal (IP) or intravenous (IV) injection, with dosages varying depending on the model. In the rat model of ventilator-induced lung injury, a dose of 0.5-1 mg/kg is used to assess pulmonary edema and inflammation. For liver ischemia-reperfusion injury in mice, the peptide's effect on IL-22/IL-22R1/STAT3 signaling is evaluated. In the mouse model of pneumococcal meningitis, the FPR2-dependent anti-inflammatory response is analyzed. Endpoints typically include histological analysis of tissue damage, measurement of inflammatory cytokine levels in serum and tissues, and assessment of clinical scores and survival rates.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic (PK) data for Ac2-26 ammonium are not extensively detailed in the available literature. As a peptide with a molecular weight of 3089.43, its PK properties would be significantly influenced by factors such as proteolytic degradation, renal clearance, and potential binding to plasma proteins. Typically, peptides are administered via injection to bypass first-pass metabolism. The stability and half-life of Ac2-26 in vivo can be modulated by its formulation and route of administration. For research purposes, the peptide is stable as a powder when stored at -20°C for up to 3 years and is soluble in water (30 mg/mL at pH 8).
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| Toxicity/Toxicokinetics |
Toxicological data for Ac2-26 ammonium are not prominently featured in the provided sources, as it is a research compound. However, given that it is a derivative of the endogenous protein Annexin-A1, its toxicity profile is expected to be favorable at therapeutic doses. In the studies reviewed, no acute toxicity or adverse effects were reported at the doses used (e.g., 0.5-1 mg/kg in rats). Standard toxicological assessments, such as acute and repeated-dose toxicity studies in rodents, would be required for a comprehensive safety evaluation. As with all research peptides, it is intended for laboratory use only and not for human consumption.
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| References |
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| Additional Infomation |
Ac2-26 ammonium (Catalog No. T78371) has a molecular weight of 3089.43 (free base) and a purity of 95.58%. Its sequence is Ac-Ala-Met-Val-Ser-Glu-Phe-Leu-Lys-Gln-Ala-Trp-Phe-Ile-Glu-Asn-Glu-Glu-Gln-Glu-Tyr-Val-Gln-Thr-Val-Lys (Ac-AMVSEFLKQAWFIENEEQEYVQTVK). The peptide is a white solid, soluble in water (30 mg/mL at pH 8), and should be stored as a powder at -20°C for long-term stability. It is a valuable tool for studying the biology of Annexin-A1 and formyl peptide receptors, with potential therapeutic applications in inflammatory diseases. While it has shown promise in preclinical models, it is not approved for clinical use and no information on clinical trials is available.
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| Molecular Formula |
C141H210N32O44S.XNH3
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| Molecular Weight |
3089.43 (free base)
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| Related CAS # |
Ac2-26;151988-33-9;Ac2-26 TFA
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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) |
H2O :~50 mg/mL
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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