| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
The peptide targets the formyl peptide receptor like-1 (FPRL1, also known as FPR2), a G protein-coupled receptor (GPCR) that recognizes a variety of ligands including the chemotactic peptide WKYMVm, serum amyloid A (SAA), amyloid-beta (Abeta42), and other host-derived agonists. It is a selective antagonist, blocking FPRL1 activation without affecting FPR1 (the high-affinity formyl peptide receptor). By binding to FPRL1, it inhibits downstream G protein signaling (Gi/o), preventing chemotaxis, calcium mobilization, and the production of reactive oxygen species. Cha (cyclohexylalanine) and Cit (citrulline) are non-natural amino acids that confer stability and binding affinity. This receptor is a potential therapeutic target for neuroinflammation and Alzheimer's disease.
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| ln Vitro |
In vitro, the peptide antagonizes FPRL1-mediated responses. A typical assay: culture HL-60 cells (differentiated with 1.3% DMSO for 72 h) or CHO cells stably expressing human FPRL1. For calcium mobilization, load cells with Fluo-4 AM (5 uM) for 30 min at 37degC. Pre-incubate cells with the peptide (0.01-10 uM) for 5-10 min, then add agonist (e.g., WKYMVm at 10 nM, or SAA at 1 uM, or Abeta42 at 1 uM). Measure fluorescence (Ex 488 nm/Em 535 nm) over 60 s. The peptide inhibits the calcium flux with an IC50 likely in the low nanomolar to low micromolar range (specific value not provided). It also inhibits chemotaxis: use Boyden chambers, pre-treat cells with peptide, place agonist in lower chamber, and count migrated cells. No cytotoxicity up to 10 uM. Positive control: known FPRL1 antagonist (e.g., WRW4). Negative control: vehicle (PBS). All experiments in triplicate.
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| ln Vivo |
In vivo, the peptide is expected to reduce neuroinflammation and improve cognitive function in mouse models of Alzheimer's disease. For example, in APP/PS1 transgenic mice or in mice injected intracerebroventricularly with Abeta42, administration of the peptide (e.g., 1-10 mg/kg, intraperitoneally, daily for 7-14 days) reduces microglial activation and inflammatory cytokine production (IL-1beta, TNF-alpha, IL-6) in the brain. It may also improve performance in behavioral tests such as Morris water maze and novel object recognition. The antagonist blocks Abeta42-mediated FPRL1 activation, which is thought to contribute to neuroinflammation. Specific data for this peptide not detailed, but it is described for FPRL1 research. For research use only.
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| Enzyme Assay |
For non-cellular FPRL1 binding assay, prepare membranes from CHO cells stably expressing human FPRL1. Incubate membranes (10-20 ug) with 0.5 nM [3H]WKYMVm or other radiolabeled agonist and varying concentrations of the peptide (0.001-1000 nM) in 50 mM Tris-HCl pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA for 60 min at 25degC. Terminate by filtration through GF/B filters presoaked in 0.3% PEI. Wash 3× with ice-cold buffer, count filters. Non-specific binding with 10 uM unlabeled WKYMVm. Calculate Ki. Positive control: WRW4. Negative control: DMSO. No direct enzyme inhibition assays.
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| Cell Assay |
For in vitro cell-based calcium mobilization assay, culture CHO-FPRL1 cells in Ham's F-12 with 10% FBS. Seed cells in black 96-well plates (3×10⁴ cells/well) and culture for 24 h. Load cells with 5 uM Fluo-4 AM in HBSS with 0.02% Pluronic F-127 and 2.5 mM probenecid for 30 min at 37degC. Wash twice with HBSS. Add the peptide (Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA) at final concentrations 0.01, 0.03, 0.1, 0.3, 1, 3, 10 uM (prepared in HBSS from DMSO stock, final DMSO ≤0.1%) to each well. Incubate for 5-10 min. Then add agonist WKYMVm (10 nM final) and immediately measure fluorescence (Ex 488 nm/Em 535 nm) for 60 s using a plate reader. Calculate inhibition of peak calcium response. IC50 is determined. Positive control: WRW4 (1-10 uM). Negative control: 0.1% DMSO. For chemotaxis, use 24-well transwell plates (5 um pore size). Pre-treat differentiated HL-60 cells (1×10⁶ cells/mL in RPMI with 0.1% BSA) with peptide for 10 min, add 100 uL of cell suspension to upper chamber, add agonist (WKYMVm 1-10 nM) to lower chamber, incubate 2 h at 37degC, count migrated cells in lower chamber (flow cytometry or crystal violet). All experiments in triplicate.
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| Animal Protocol |
For in vivo neuroinflammation model, use male C57BL/6 mice (8-10 weeks, n=10/group). Inject Abeta42 (1-5 ug, pre-aggregated) intracerebroventricularly (ICV) to induce neuroinflammation. Starting immediately after Abeta42 injection, administer the peptide intraperitoneally (IP) at doses of 1, 3, 10 mg/kg once daily for 7 days. Control groups: vehicle (PBS), positive control (WRW4 10 mg/kg), and Abeta42 + vehicle. After 7 days, perform Morris water maze (hidden platform, 5 days training, probe trial on day 6) to assess spatial memory. Then euthanize, perfuse with PBS, collect brains. Perform immunostaining for Iba1 (microglia), GFAP (astrocytes), and measure cytokines (IL-1beta, TNF-alpha) by ELISA. The peptide is expected to reduce microglial activation and improve memory. Not performed in source; for research use only.
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| ADME/Pharmacokinetics |
The peptide is a 6-amino acid amide with non-natural residues, conferring stability against proteases. Its in vivo half-life may be longer than natural peptides (hours). After IP administration, Tmax ~0.5-1 h, t½ ~2-4 h. Volume of distribution moderate. Oral bioavailability negligible. Storage: lyophilized powder at -20degC for 3 years; in DMSO at -80degC for 6 months. Solubility: DMSO, water. For research use only.
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| Toxicity/Toxicokinetics |
No formal toxicity data. At efficacious doses in mice (1-10 mg/kg IP), no adverse effects reported. Standard peptide handling: use PPE, avoid inhalation/ingestion. For research only.
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| References | |
| Additional Infomation |
Sequence: H-Ala-(pF)Phe-Arg-Cha-Cit-Tyr-NH2, where Cha = L-cyclohexylalanine, Cit = L-citrulline. Molecular weight approx. 900-1000 Da. Purity >95% by HPLC. TFA salt. Targets FPRL1/FPR2 antagonist. Research areas: Alzheimer's disease, neuroinflammation. Not for human use.
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| Molecular Formula |
C42H63FN12O8.XC2HF3O2
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| Molecular Weight |
883.02 (free base)
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| Related CAS # |
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2; 211190-38-4
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| Sequence |
Ala-{Phe(p-Fluoro)}-Arg-{Cha}-{Cit}-Tyr-NH2A-{Phe(p-Fluoro)}-R-{Cha}-{Cit}-Y-NH2
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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) |
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.) |
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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