GLPBio

WRW4

Catalog No.: GC10691Purity:>99.50%
COASDSData Sheet
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.

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WRW4
Cas No.: 878557-55-2
1mgIn Stock
$48.00
1
5mgIn Stock
$108.00
1
10mgIn Stock
$168.00
1
25mgIn Stock
$320.00
1
50mgIn Stock
$480.00
1
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Description

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.

Protocol

Cell experiment [1]:

Cell lines

 Organotypic hippocampal cultures (OHCs)

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.

Reaction Conditions

 10µM; 30min

Applications

 WRW4 reverses the potential of MR-39 to alleviate Aβ-induced inflammatory response in OHCs.
Animal experiment [2]:

Animal models

 C57BL/6 mice

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.

Dosage form

 10µg, 0.1mL; i.p.

Applications

 WRW4 reverses the anti-inflammatory effect of WKYMV.

References:
[1] 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.
[2]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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
878557-55-2
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-
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
Molecular Formula
C61H65N15O6
Molecular Weight
1104.28
Solubility
Soluble to 1 mg/ml in Water
Storage
Desiccate at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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