WRW4 |
Catalog No.GC10691
One-Click Copy Product Info
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WRW4 is a selective antagonist of formyl peptide receptor 2 (FPR2, formerly known as FPRL1), which is a synthetic C-terminal amidated hexapeptide, its IC50 value for inhibiting the binding of WKYMVm to FPRL2 is 0.23 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 878557-55-2
Sample solution is provided at 25 µL, 10mM.
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WRW4 is a selective antagonist of formyl peptide receptor 2 (FPR2, formerly known as FPRL1), which is a synthetic C-terminal amidated hexapeptide, its IC50 value for inhibiting the binding of WKYMVm to FPRL2 is 0.23 μM[1, 2]. WRW4 can inhibit intracellular calcium release and ERK phosphorylation induced by FPR2 agonists (such as WKYMVm, MMK‑1, Aβ42, and F peptide), thereby suppressing downstream responses such as chemotaxis, peroxide production, and Aβ42 internalization[3, 4]. WRW4 can alleviate cognitive decline caused by diabetes in mice[5].
In vitro, pretreatment of organotypic hippocampal cultures (OHCs) with WRW4 (10µM) for 30min reversed the anti-inflammatory effect of MR-39 on Aβ-induced inflammation in OHCs[6].
In vivo, WRW4 (10µg, 0.1mL) reversed the anti-inflammatory effect of WKYMV by intraperitoneal injection in mice with experimental peritonitis[7].
References:
[1] Skovbakke, Sarah L., et al. The role of formyl peptide receptors for immunomodulatory activities of antimicrobial peptides and peptidomimetics. Current pharmaceutical design 24.10 (2018): 1100-1120.
[2] Shin, Eun Ha, et al. Trp-Arg-Trp-Trp-Trp-Trp antagonizes formyl peptide receptor like 2-mediated signaling. Biochemical and biophysical research communications 341.4 (2006): 1317-1322.
[3] Bae, Yoe-Sik, et al. Identification of peptides that antagonize formyl peptide receptor-like 1-mediated signaling.The Journal of Immunology 173.1 (2004): 607-614.
[4] Cattaneo, Fabio, Melania Parisi, and Rosario Ammendola. Distinct signaling cascades elicited by different formyl peptide receptor 2 (FPR2) agonists. International journal of molecular sciences 14.4 (2013): 7193-7230.
[5] Uno, Hiroki, Takahide Itokazu, and Toshihide Yamashita. Formyl peptide receptor 2 antagonist WRW4 ameliorates diabetes-induced cognitive decline in mice.Neuroscience Research (2025): 104932.
[6] Trojan, Ewa, et al. The N-formyl peptide receptor 2 (FPR2) agonist MR-39 improves ex vivo and in vivo amyloid beta (1–42)-induced neuroinflammation in mouse models of Alzheimer’s disease. Molecular neurobiology 58.12 (2021): 6203-6221.
[7] Lice, Izabella, et al. Effects of formyl peptide receptor agonists ac9-12 and WKYMV in in vivo and in vitro acute inflammatory experimental models. Cells 11.2 (2022): 228.
| Cell experiment [1]: | |
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Cell lines |
Organotypic hippocampal cultures (OHCs) |
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Preparation Method |
OHCs obtained from WT and KO FPR2−/−mice were pretreated for 30min with the FPR2 antagonist WRW4 (10µM). Then, MR-39 (1µM) was added for 1h, and OHCs were stimulated for 24h with fibrillary or oligomeric amyloid β (Aβ1-42; 10μM). Control (unstimulated) OHCs were treated with PBS. |
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Reaction Conditions |
10µM; 30min |
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Applications |
WRW4 reverses the potential of MR-39 to alleviate Aβ-induced inflammatory response in OHCs. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
Animals were distributed in 8 experimental groups: Control, Carrageenan (CG), pre- or post-treated with Ac9-12 or WKYMV, pre-treated with WRW4+Ac9-12 or WRW4+WKYMV. Peritonitis was induced by intraperitoneal (i.p.) injection of 1.0mL of 0.3% carrageenan solution diluted in sterile saline, whereas control mice received saline solution only. To determine the therapeutic efficacy of the synthetic peptides in this model, mice received carrageenan by i.p. 15min before or after i.p. peptide treatments (100µg/animal of Ac9-12 or WKYMV with or without WRW4 at 10µg/animal) diluted in 0.1mL of saline solution. After 3h, the animals were euthanized to collect the peritoneal lavage. |
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Dosage form |
10µg, 0.1mL; i.p. |
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Applications |
WRW4 reverses the anti-inflammatory effect of WKYMV. |
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References: |
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| Cas No. | 878557-55-2 | SDF | |
| Chemical Name | (S,Z)-2-((Z)-((S)-2-amino-1-hydroxy-3-(1H-indol-3-yl)propylidene)amino)-5-guanidino-N-((S,Z)-1-hydroxy-1-(((S,Z)-1-hydroxy-1-(((S,Z)-1-hydroxy-1-(((S)-1-hydroxy-1-imino-3-(1H-indol-3-yl)propan-2-yl)imino)-3-(1H-indol-3-yl)propan-2-yl)imino)-3-(1H-indol-3- | ||
| Canonical SMILES | N[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC1=CNC2=CC=CC=C12)([H])CC3=CNC4=CC=CC=C34)([H])CC5=CNC6=CC=CC=C56)([H])CC7=CNC8=CC=CC=C78)([H])CCCNC(N)=N)([H])CC9=CNC%10=CC=CC=C9%10 | ||
| Formula | C61H65N15O6 | M.Wt | 1104.28 |
| Solubility | Soluble to 1 mg/ml in Water | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 905.6 μL | 4.5278 mL | 9.0557 mL |
| 5 mM | 181.1 μL | 905.6 μL | 1.8111 mL |
| 10 mM | 90.6 μL | 452.8 μL | 905.6 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)