| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
N-Formyl-Met-Leu-Phe-Lys targets the formyl peptide receptor 1 (FPR1) with high selectivity and potency. It acts as a potent and selective agonist of FPR1, with an EC₅₀ of 3.5 nM for this receptor. It has significantly lower activity at FPR2 (EC₅₀ = 6.7 μM) and the FPR2-D2817.32G variant (EC₅₀ = 0.88 μM). By binding to FPR1 on phagocytic leukocytes, the peptide activates downstream signaling pathways that lead to chemotaxis and the respiratory burst.
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| ln Vitro |
In vitro, N-Formyl-Met-Leu-Phe-Lys acts as a potent and selective agonist of FPR1, with EC₅₀ values of 3.5 nM for FPR1, 6.7 μM for FPR2, and 0.88 μM for FPR2-D2817.32G. Its primary activity is the stimulation of immune responses, particularly the activation and chemotaxis of leukocytes. The peptide's high potency and selectivity for FPR1 make it a standard tool for studying FPR1-mediated signaling in phagocytes.
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| ln Vivo |
In vivo, N-Formyl-Met-Leu-Phe-Lys is used to study the innate immune response by inducing leukocyte recruitment and activation. Its role as a potent chemoattractant for phagocytic leukocytes is crucial for understanding how the immune system responds to bacterial infections. It is a standard tool for inducing a localized inflammatory response in animal models to study the dynamics of immune cell infiltration.
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| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for N-Formyl-Met-Leu-Phe-Lys typically involve radioligand binding studies using membranes from cells expressing FPR1, FPR2, or their variants. The peptide's affinity and selectivity are determined by competitive displacement of a radiolabeled formyl peptide probe. Functional assays measure receptor activation by monitoring downstream signaling, such as calcium flux or GTPγS binding.
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| Cell Assay |
In vitro cell-based assays for N-Formyl-Met-Leu-Phe-Lys use phagocytic leukocytes (e.g., neutrophils) or cell lines expressing FPR1. Cells are treated with the peptide, and activation is assessed by measuring chemotaxis (using Boyden chambers), calcium mobilization (using fluorescent dyes), or the respiratory burst (by measuring superoxide production). These assays quantify the peptide's potency as a chemoattractant and activator of immune cells.
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| Animal Protocol |
In vivo animal studies for N-Formyl-Met-Leu-Phe-Lys typically involve administering the peptide to rodents to induce a localized inflammatory response. This can be done by injection into a specific tissue (e.g., peritoneum, air pouch) or by systemic administration. The resulting leukocyte infiltration is quantified by counting cells in the lavage fluid or by histological examination of the tissue. These models are used to study the mechanisms of leukocyte recruitment and inflammation.
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| ADME/Pharmacokinetics |
N-Formyl-Met-Leu-Phe-Lys has a molecular weight of 565.73 g/mol and a molecular formula of C₂₇H₄₃N₅O₆S. As a peptide, it is expected to have poor oral bioavailability and a short half-life in vivo due to rapid degradation by peptidases. Its primary application is as a research tool for in vitro and in vivo studies of FPR1-mediated signaling and immune cell function.
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| Toxicity/Toxicokinetics |
The toxicity of N-Formyl-Met-Leu-Phe-Lys is primarily related to its potent inflammatory activity. At high doses, it can cause a severe systemic inflammatory response. However, when used at appropriate concentrations in research settings, it is a standard and well-tolerated tool for studying immune cell activation. Comprehensive toxicological data are limited as it is not a therapeutic agent.
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| References | |
| Additional Infomation |
N-Formyl-Met-Leu-Phe-Lys (fMLFK) is a well-characterized synthetic peptide that serves as a potent and selective agonist of the formyl peptide receptor 1 (FPR1). It is a standard research tool used extensively to study the mechanisms of leukocyte chemotaxis, activation, and the innate immune response. Its high potency and selectivity make it invaluable for investigating FPR1 signaling pathways. Not approved for clinical use; intended for research purposes only.
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| Molecular Formula |
C27H43N5O6S
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|---|---|
| Molecular Weight |
565.72522
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| Exact Mass |
565.293
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| CAS # |
67247-11-4
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| PubChem CID |
9894161
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| Appearance |
White to off-white solid powder
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| LogP |
3.71
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
39
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| Complexity |
778
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CCSC)NC=O
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| InChi Key |
OERILMBTPCSYNG-MLCQCVOFSA-N
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| InChi Code |
InChI=1S/C27H43N5O6S/c1-18(2)15-22(31-24(34)20(29-17-33)12-14-39-3)25(35)32-23(16-19-9-5-4-6-10-19)26(36)30-21(27(37)38)11-7-8-13-28/h4-6,9-10,17-18,20-23H,7-8,11-16,28H2,1-3H3,(H,29,33)(H,30,36)(H,31,34)(H,32,35)(H,37,38)/t20-,21-,22-,23-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]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 |
| 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
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7676 mL | 8.8381 mL | 17.6763 mL | |
| 5 mM | 0.3535 mL | 1.7676 mL | 3.5353 mL | |
| 10 mM | 0.1768 mL | 0.8838 mL | 1.7676 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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