| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Targets the formyl peptide receptor (FPR), specifically FPR1, as an agonist. FPR1 is a GPCR involved in the regulation of innate immunity. By binding to FPR1, Ac9-25 activates a potent pro-inflammatory program in neutrophils, leading to their activation and the production of microbicidal oxygen species.
|
|---|---|
| ln Vitro |
Ac9-25 has been shown to potently stimulate neutrophil NADPH oxidase activity through activation of the FPR. This results in a "respiratory burst," characterized by the rapid production of superoxide and other reactive oxygen species (ROS). This in vitro activity is a key endpoint for characterizing FPR agonists and understanding their role in the innate immune response.
|
| ln Vivo |
Detailed in vivo activity data for Ac9-25 is limited. As an N-terminal peptide of Annexin I, which is an endogenous anti-inflammatory protein, the Ac9-25 peptide has been shown to mimic some of these effects. It is known to inhibit leukocyte extravasation, the process by which white blood cells leave the bloodstream to enter inflamed tissues, suggesting a role in modulating the inflammatory response.
|
| Enzyme Assay |
No cell-free, non-cell assay data is available for this peptide agonist. Its activity is mediated by binding to a cell-surface GPCR on neutrophils, which initiates a complex intracellular signaling cascade. This process cannot be studied in a simple non-cell assay; functional assays require intact, living cells to measure downstream effects like ROS production.
|
| Cell Assay |
The functional activity of Ac9-25 is typically assessed using primary human neutrophils. The neutrophils are isolated from whole blood and treated with the peptide. The production of superoxide (a measure of NADPH oxidase activation) is then measured using a colorimetric assay, such as the reduction of ferricytochrome c, or a chemiluminescence-based method. This provides a quantitative readout of the peptide‘s activity.
|
| Animal Protocol |
No specific animal studies for Ac9-25 are publicly available. For an in vivo study exploring its anti-inflammatory effects, a common model is the murine air-pouch or a model of carrageenan-induced paw edema. Ac9-25 could be administered systemically or locally, and endpoints would include measuring the number of infiltrating leukocytes, levels of inflammatory cytokines, and tissue swelling.
|
| ADME/Pharmacokinetics |
Detailed PK data for Ac9-25 is not publicly available. As a peptide, it is expected to be rapidly degraded by proteases in vivo, leading to a very short half-life. It is typically used in in vitro experiments. Its molecular weight is 2183.33 g/mol, and it is quite large, which would limit its oral bioavailability and require injection for in vivo administration.
|
| Toxicity/Toxicokinetics |
No toxicity data is publicly available for Ac9-25. As a peptide derived from an endogenous protein and used at low concentrations in research, significant toxicity is not expected. However, its ability to activate the NADPH oxidase in neutrophils could, in principle, lead to tissue damage if it induces a strong, uncontrolled inflammatory response in vivo.
|
| References |
|
| Additional Infomation |
Ac9-25 is a research-grade peptide and is not approved for clinical use. It serves as a valuable tool to study the role of FPR1 in neutrophil biology and inflammation. Interestingly, while the parent protein Annexin I is anti-inflammatory, this N-terminal peptide acts as an FPR agonist, highlighting the complex biology of Annexin I-derived peptides.
|
| Molecular Formula |
C99H143N23O33
|
|---|---|
| Molecular Weight |
2183.33
|
| Exact Mass |
320.185
|
| CAS # |
284040-76-2
|
| Related CAS # |
Ac9-25 TFA
|
| PubChem CID |
62286
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.889
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
444
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KCTKQZUYHSKJLP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H15N3O3.C3H9N/c1-7(2)13(3)12(19)15-10(16-13)9-8(11(17)18)5-4-6-14-9;1-3(2)4/h4-7H,1-3H3,(H,17,18)(H,15,16,19);3H,4H2,1-2H3
|
| Chemical Name |
2-(4-methyl-5-oxo-4-propan-2-yl-1H-imidazol-2-yl)pyridine-3-carboxylic acid;propan-2-amine
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4580 mL | 2.2901 mL | 4.5802 mL | |
| 5 mM | 0.0916 mL | 0.4580 mL | 0.9160 mL | |
| 10 mM | 0.0458 mL | 0.2290 mL | 0.4580 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.