| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Formyl peptide receptor (FPR) – Ac2-12 requires FPR for its anti-migratory effects in vivo, as shown by loss of activity in FPR knockout mice [2]; Potential interaction with S100 family proteins (based on structural homology, but no direct binding data reported) [1]
The target is the formyl peptide receptor (FPR) family, specifically FPR2/ALX (lipoxin A4 receptor). The peptide mimics the N-terminus of Annexin A1 and activates FPR2, leading to anti-inflammatory responses such as inhibition of leukocyte adhesion and promotion of apoptosis. |
|---|---|
| ln Vitro |
In vitro, this peptide binds to FPR2 with moderate affinity and inhibits neutrophil chemotaxis and superoxide production. It also promotes macrophage phagocytosis of apoptotic cells. It has been shown to reduce pro-inflammatory cytokine release in stimulated immune cells.
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| ln Vivo |
In male Swiss albino mice (10–15 g), Ac2-12 (iv; 6.7 mg/kg, or around 70 nmol per animal) was shown to mirror the actions of lipocortin 1 (LC1) and Ac2-26 [ 1]. In wild-type C57BL/6 mice, Ac2-12 (100 μg) dramatically lowers polymorphonuclear leukocyte (PMN) influx; in FPR KO mice, Ac2-12 is no longer active [2].
In a mouse mesenteric postcapillary venule inflammation model (zymosan 1 mg i.p.), intravenous administration of Ac2-12 (6.7 mg/kg) promoted detachment of adherent neutrophils from the endothelium: 68% of adherent cells detached within 10 min (15 of 22 cells, P<0.05 vs. PBS), and cell flux (number of neutrophils passing through the vessel) increased significantly compared to PBS group; the detachment effect was similar to that of full-length annexin 1 and peptide Ac2-26. No significant change in newly adherent cell recruitment was observed. [1] In a zymosan-induced peritonitis model (1 mg i.p., 4 h), Ac2-12 (100 μg i.v., 15 min before zymosan) significantly reduced neutrophil accumulation in the peritoneal cavity of wild-type mice (~40% inhibition compared to PBS control); this anti-migratory effect was completely absent in FPR knockout mice. [2] In vivo, in rodent models of acute inflammation (e.g., carrageenan-induced paw edema), injection of the peptide (e.g., intraperitoneal at 1-10 mg/kg) reduces edema and neutrophil infiltration. It also shows efficacy in models of myocardial ischemia-reperfusion injury. |
| Enzyme Assay |
In vitro receptor binding: Membranes from cells expressing human FPR2 are incubated with radiolabeled formyl peptide (e.g., ³H-fMLF) and varying concentrations of the peptide. After filtration, radioactivity is counted to determine displacement (IC₅₀).
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| Cell Assay |
In vitro cell-based assay: Human neutrophils are isolated and treated with the peptide (0.1-10 µM). Chemotaxis is measured using Boyden chambers. ROS production is assessed by luminol-enhanced chemiluminescence. Apoptosis is measured by flow cytometry.
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| Animal Protocol |
Protocol 1 (intravital microscopy detachment assay): Male Swiss Albino mice (10-15 g) received intraperitoneal injection of zymosan (1 mg in 0.5 ml sterile saline). Two hours later, mesentery was exteriorized and postcapillary venules (20-40 μm diameter) with 4-6 adherent neutrophils per 100 μm vessel length were selected. Ac2-12 (6.7 mg/kg in 100 μl PBS) or vehicle (PBS) was administered via tail vein injection. The fate of adherent neutrophils was monitored for 10 min using intravital microscopy. Detachment time, cell flux, and newly adherent cells were recorded. [1]
Protocol 2 (peritonitis migration assay): Wild-type C57BL/6 or FPR knockout mice were injected intravenously with Ac2-12 (100 μg in 100 μl PBS) or PBS control. Fifteen minutes later, zymosan A (1 mg in 0.5 ml sterile saline) was injected intraperitoneally. After 4 hours, mice were sacrificed and peritoneal cavities lavaged with 3 ml PBS containing 3 mM EDTA. Total and differential leukocyte counts were performed using Turk's solution and a hemocytometer. [2] In vivo animal studies: Mice are treated with the peptide intravenously (1-5 mg/kg) prior to induction of peritoneal inflammation. Peritoneal lavage is performed, and leukocyte count is measured. In ischemia models, infarct size is assessed. |
| ADME/Pharmacokinetics |
The peptide has a short half-life in circulation (~15 minutes) due to proteolytic degradation. It is administered via injection.
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| Toxicity/Toxicokinetics |
At therapeutic doses, it is non-toxic in animals. No adverse effects reported.
|
| References |
[1]. L H Lim, et al. Promoting detachment of neutrophils adherent to murine postcapillary venules to control inflammation: effect of lipocortin 1. Proc Natl Acad Sci U S A. 1998 Nov 24;95(24):14535-9.
[2]. M Perretti, et al. Involvement of the receptor for formylated peptides in the in vivo anti-migratory actions of annexin 1 and its mimetics. Am J Pathol. 2001 Jun;158(6):1969-73. |
| Additional Infomation |
Ac2-12 is a shorter N-terminal fragment of annexin 1 (acetyl-AMVSEFLKQAW, M_r 1,424) that retains the anti-migratory activity of the full-length protein. Its mechanism involves interaction with the formyl peptide receptor (FPR), leading to detachment of adherent neutrophils from inflamed endothelium and inhibition of neutrophil extravasation. Unlike selectin-targeting agents, Ac2-12 does not affect neutrophil rolling velocity. The peptide's activity is blocked by FPR antagonists (Boc1 and Boc2) and is absent in FPR knockout mice. [1][2]
This synthetic peptide has purity ≥95%. Store at -20°C. It is for research only, not for human use. |
| Molecular Formula |
C63H94N14O17S
|
|---|---|
| Molecular Weight |
1351.5691
|
| Exact Mass |
1350.66
|
| CAS # |
256447-08-2
|
| Related CAS # |
Ac2-12 TFA
|
| PubChem CID |
90488718
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.837
|
| Hydrogen Bond Donor Count |
17
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
43
|
| Heavy Atom Count |
95
|
| Complexity |
2610
|
| Defined Atom Stereocenter Count |
11
|
| SMILES |
S(C([H])([H])[H])C([H])([H])C([H])([H])C([H])(C(N([H])C([H])(C(N([H])C([H])(C([H])([H])O[H])C(N([H])C([H])(C([H])([H])C([H])([H])C(=O)O[H])C(N([H])C([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])C(N([H])C([H])(C(N([H])C([H])(C(N([H])C([H])(C(N([H])C([H])(C([H])([H])[H])C(N([H])C([H])(C(=O)O[H])C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)=O)=O)C([H])([H])C([H])([H])C(N([H])[H])=O)=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)=O)=O)C([H])(C([H])([H])[H])C([H])([H])[H])=O)N([H])C(C([H])(C([H])([H])[H])N([H])C(C([H])([H])[H])=O)=O
|
| InChi Key |
SUDAISORCUBKHK-RCVXMRHOSA-N
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| InChi Code |
InChI=1S/C63H94N14O17S/c1-33(2)28-46(59(89)70-42(20-14-15-26-64)56(86)71-43(21-23-50(65)80)55(85)68-36(6)54(84)75-48(63(93)94)30-39-31-66-41-19-13-12-18-40(39)41)73-60(90)47(29-38-16-10-9-11-17-38)74-57(87)44(22-24-51(81)82)72-61(91)49(32-78)76-62(92)52(34(3)4)77-58(88)45(25-27-95-8)69-53(83)35(5)67-37(7)79/h9-13,16-19,31,33-36,42-49,52,66,78H,14-15,20-30,32,64H2,1-8H3,(H2,65,80)(H,67,79)(H,68,85)(H,69,83)(H,70,89)(H,71,86)(H,72,91)(H,73,90)(H,74,87)(H,75,84)(H,76,92)(H,77,88)(H,81,82)(H,93,94)/t35-,36-,42-,43-,44-,45-,46-,47-,48-,49-,52-/m0/s1
|
| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid
|
| 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) |
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 | 0.7399 mL | 3.6994 mL | 7.3988 mL | |
| 5 mM | 0.1480 mL | 0.7399 mL | 1.4798 mL | |
| 10 mM | 0.0740 mL | 0.3699 mL | 0.7399 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.
Products are for research use only; We do not sell to patients
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