| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
WRW4 specifically targets the FPRL1 receptor, also known as FPR2, a G protein-coupled receptor involved in the regulation of inflammatory responses, chemotaxis, and the resolution of inflammation. It acts as a competitive antagonist, inhibiting the binding of the high-affinity agonist WKYMVm to FPRL1 with an IC50 of 0.23 μM. WRW4 effectively blocks the activation of this receptor by other agonists.
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| ln Vitro |
WRW4 totally prevents Abeta42 peptide uptake in human macrophages and also suppresses Abeta42 peptide-induced neutrophil superoxide generation and chemotactic movement. Through WKYMVm, WRW4 selectively prevents ERK phosphorylation downstream of FPRL1 [1].
In vitro, WRW4 specifically inhibits FPRL1-mediated cellular responses. It completely inhibits the increase in intracellular calcium, the activation of extracellular signal-regulated kinase (ERK), and the chemotactic migration of cells towards the agonist WKYMVm. It also specifically inhibits the increase in intracellular calcium induced by other FPRL1 agonists, such as MMK-1, the amyloid beta42 (Abeta42) peptide, and the F peptide. |
| ln Vivo |
In vivo activity data for WRW4 are not extensively detailed in the provided search results. As a specific antagonist of FPR2/FPRL1, it is a critical research tool for investigating the role of this receptor in various inflammatory and neurological disease models. It is used to block FPR2 signaling in vivo to study its function in conditions such as neuroinflammation and ischemic injury, but specific in vivo protocols are not detailed.
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| Enzyme Assay |
For non-cellular in vitro enzyme/receptor binding assays, WRW4 is used to characterize its binding affinity and antagonistic properties at the FPRL1 receptor. Typically, this involves radioligand binding displacement assays, where the ability of WRW4 to compete with a labeled agonist, such as [125I]-WKYMVm, for binding to the receptor is measured. The IC50 value of 0.23 μM is determined in such assays.
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| Cell Assay |
For in vitro cellular assays, the activity of WRW4 is evaluated in cells expressing the FPRL1 receptor. A typical assay involves measuring the inhibition of agonist-induced intracellular calcium mobilization. Cells are loaded with a calcium-sensitive fluorescent dye, and the increase in fluorescence upon addition of an agonist like WKYMVm is measured. WRW4 is added prior to the agonist to assess its ability to block this response.
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| Animal Protocol |
In vivo animal studies with WRW4 are typically conducted in mouse models of inflammatory diseases, neuroinflammation, or cancer. For example, it may be administered to mice to block FPR2 signaling in models of acute lung injury, colitis, or Alzheimer's disease to study the receptor's role in disease pathogenesis. The compound can be administered via various routes, including intraperitoneal or intracerebroventricular injection, depending on the target organ or disease model.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for WRW4 are not extensively documented. As a peptide, its oral bioavailability is likely low, and it would require parenteral administration for in vivo studies. Its stability in biological fluids and its half-life would be key parameters for consideration in experimental design. The compound is soluble in DMSO at 100 mg/mL and in water at 50 mg/mL, which aids in formulation for both in vitro and in vivo applications.
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| Toxicity/Toxicokinetics |
Toxicological data for WRW4 are limited. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
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| References | |
| Additional Infomation |
FPRL2 antagonists
WRW4 is a specific and potent antagonist of the formyl peptide receptor-like 1 (FPRL1/FPR2). It inhibits WKYMVm binding with an IC50 of 0.23 μM and blocks downstream signaling, including calcium mobilization, ERK activation, and chemotaxis. It also inhibits responses to other agonists like MMK-1 and Aβ42. WRW4 is a key tool compound for studying FPR2-mediated immune and inflammatory pathways. |
| Molecular Formula |
C61H65N15O6
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|---|---|
| Molecular Weight |
1104.27
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| Exact Mass |
1103.52
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| CAS # |
878557-55-2
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| Related CAS # |
WRW4 TFA
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| PubChem CID |
49768327
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| Appearance |
White to off-white solid powder
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| LogP |
8.652
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
25
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| Heavy Atom Count |
82
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| Complexity |
2220
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C1=CC=C2C(=C1)C(=CN2)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC7=CNC8=CC=CC=C87)C(=O)N[C@@H](CC9=CNC1=CC=CC=C19)C(=O)N)N
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| InChi Key |
IRJDOVLLPORVJP-WOAIKHIASA-N
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| InChi Code |
InChI=1S/C61H65N15O6/c62-44(24-34-29-67-45-17-6-1-12-39(34)45)56(78)72-50(22-11-23-66-61(64)65)57(79)74-53(27-37-32-70-48-20-9-4-15-42(37)48)59(81)76-54(28-38-33-71-49-21-10-5-16-43(38)49)60(82)75-52(26-36-31-69-47-19-8-3-14-41(36)47)58(80)73-51(55(63)77)25-35-30-68-46-18-7-2-13-40(35)46/h1-10,12-21,29-33,44,50-54,67-71H,11,22-28,62H2,(H2,63,77)(H,72,78)(H,73,80)(H,74,79)(H,75,82)(H,76,81)(H4,64,65,66)/t44-,50-,51-,52-,53-,54-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-5-(diaminomethylideneamino)pentanamide
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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 (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) |
DMSO: 100 mg/mL (90.56 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (2.26 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (2.26 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 | 0.9056 mL | 4.5279 mL | 9.0558 mL | |
| 5 mM | 0.1811 mL | 0.9056 mL | 1.8112 mL | |
| 10 mM | 0.0906 mL | 0.4528 mL | 0.9056 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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