| 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 |
FPR/FPRL1[1]
Boc-MLF TFA targets the formyl peptide receptor 1 (FPR1), a G protein-coupled receptor primarily expressed on neutrophils and other phagocytic leukocytes. At higher concentrations, it can also inhibit signaling through the related formyl peptide receptor like-1 (FPRL1). By binding to the FPR1 orthosteric site, Boc-MLF acts as a pure antagonist, competitively inhibiting the binding of bacterial formyl peptides (like fMLF) and thereby blocking downstream pro-inflammatory signaling cascades. |
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| ln Vitro |
Boc-MLF suppresses the generation of superoxide in neutrophils when the FPR agonist fMLF is present with an EC50 of 630 nM [1]. Serum amyloid A (SAA), an FPRL1 agonist, causes a calcium response that is blocked by Boc-MLF (25 μM) [1].
In vitro, Boc-MLF inhibits superoxide production induced by the FPR1 agonist fMLF with an EC50 of 630 nM in human neutrophils. It also blocks FPRL1-agonist serum amyloid A (SAA)-induced calcium responses at a concentration of 25 microM. The compound demonstrates no agonist activity, producing 0% superoxide production, and maintains high selectivity, confirming its utility as a pure antagonist for dissecting FPR1-specific signaling pathways. |
| ln Vivo |
In vivo, the specific activity of Boc-MLF TFA has not been extensively detailed in the available literature. Its primary application is as an ex vivo or in vitro tool for studying neutrophil function. While it could be used in animal models of inflammation to block FPR1-mediated neutrophil recruitment, such studies are not routinely described. A dose of 1-10 mg/kg in mouse models could serve as a hypothetical starting point for research.
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| Enzyme Assay |
Non-cellular binding experiments are performed using radioligand binding assays with human neutrophils or FPR1-overexpressing cell membranes. The compound is used as a "cold" competitor in assays with [3H]-formyl-Nle-Leu-Phe-Nle-Tyr-Lys ([3H]-fMLF). Various concentrations of Boc-MLF are incubated with the membrane preparation and a fixed concentration of the radioligand. Following incubation and filtration, bound radioactivity is measured to calculate the inhibitory constant (Ki).
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| Cell Assay |
In vitro cellular assays involve isolating human neutrophils from whole blood. Neutrophils are pre-incubated with various concentrations of Boc-MLF (typically 1-30 microM) for 15 minutes before stimulation with fMLF. Functional endpoints include measuring superoxide anion production via cytochrome c reduction, quantifying chemotaxis using Boyden chambers, and assessing intracellular calcium flux using fluorescent dyes like Fura-2 AM. Cytotoxicity at 30 microM is minimal, with >95% viability, ensuring assay specificity.
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| Animal Protocol |
Detailed in vivo animal experimental protocols for Boc-MLF TFA are not standard in the literature. A protocol for investigating its in vivo effects could involve administering the compound via intraperitoneal (IP) injection to mice at 1-10 mg/kg before inducing peritonitis or lung inflammation with an fMLF analog. Bronchoalveolar lavage fluid (BALF) would then be analyzed for neutrophil recruitment. Such studies would help validate FPR1's role in disease models.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic (PK) studies for Boc-MLF TFA are not available in standard literature. As a small N-blocked tripeptide (M.W. 509.66 free base), it would likely have poor oral bioavailability and a short half-life in serum unless specifically modified. Its use is currently confined to in vitro assays, and further PK characterization would be required for any potential in vivo applications.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Boc-MLF TFA are not provided in standard product literature. As a research-use compound, standard safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not described. For laboratory use, standard chemical safety precautions for handling peptides should be followed. The compound shows good tolerability in isolated neutrophils with >95% viability at 30 microM.
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| References | |
| Additional Infomation |
Boc-MLF TFA (CAS: 67247-12-5 free base) has a molecular formula of C27H40F3N3O8S and a molecular weight of 623.7 g/mol as the TFA salt. It is a specific antagonist of FPR1 with a Ki of 0.23 microM. As an N-blocked tripeptide, it represents a well-established pharmacological tool that is widely used as a negative control in chemotaxis and inflammation studies to dissect FPR1-specific signaling. This product is intended for research purposes only.
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| Molecular Formula |
C27H40F3N3O8S
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|---|---|
| Molecular Weight |
623.68
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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, 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)
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| Solubility (In Vitro) |
DMSO :~150 mg/mL (~240.51 mM)
H2O :< 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6034 mL | 8.0169 mL | 16.0339 mL | |
| 5 mM | 0.3207 mL | 1.6034 mL | 3.2068 mL | |
| 10 mM | 0.1603 mL | 0.8017 mL | 1.6034 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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