WRW4

Catalog No.S9818 Batch:S981801

Technical Data

Formula

C₆₁H₆₅N₁₅O₆

Molecular Weight

1104.27

CAS No.

878557-55-2

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (90.55 mM)

Water

50 mg/mL (45.27 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.8mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

WRW4 is a specific formyl peptide receptor-like 1 (FPRL1) antagonist that inhibits WKYMVm binding to FPRL1 with IC50 of 0.23 μM. WRW4 is a selective antagonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX).

Targets

FPRL1 ^[1]
(Cell-free assay)

0.23 μM

In vitro

WRW4 shows potent activity in terms of inhibiting WKYMVm binding to FPRL1. WRW4 inhibits the activation of FPRL1 by WKYMVm, resulting in the complete inhibition of the intracellular calcium increase, extracellular signal-regulated kinase activation, and chemotactic migration of cells toward WKYMVm. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid β42 (Aβ42) peptide, and F peptide, but not by the FPR agonist, fMLF. Aβ42 peptide-induced superoxide generation and chemotactic migration of neutrophils are inhibited by WRW4, which also completely inhibits the internalization of Aβ42 peptide in human macrophages.^[1]

In vivo

Male Swiss mice undergo intraplantar (i.pl.) injection with complete Freund’s adjuvant (CFA). WRW4 prevents the antihyperalgesic effect induced by either EA or BML-111. EA increases ANXA1 but does not alter FPR2/ALX receptor levels in the paw. Furthermore, i.pl. pretreatment with WRW4 prevents the increase of ANXA1 levels induced by EA.^[2]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines RBL-2H3 cells Concentrations 10 μM Incubation Time 30 min Method To determine whether WRW4 binds to FPRL1, FPRL1-expressing RBL-2H3 cells are labeled with 10 μM biotin-WRW4 for 30 min in PBS containing 0.02% sodium azide. The unbound biotin-WRW4 is washed extensively with PBS containing 0.2% BSA and 0.02% sodium azide. Then the cells are incubated with 5 μg/ml streptavidin-FITC at 4°C for 40 min in the dark. Subsequently, cells are washed twice in washing solution and fixed with 0.2% paraformaldehyde. Fixed cells are analyzed in single laser for FITC with FACSCalibur.
Animal Study:^{^[2]}	Animal Models male Swiss mice Dosages 10 μg/paw Administration Intraplantar injection

Cell Assay:^{^[1]}

Cell lines
RBL-2H3 cells
Concentrations
10 μM
Incubation Time
30 min
Method
To determine whether WRW4 binds to FPRL1, FPRL1-expressing RBL-2H3 cells are labeled with 10 μM biotin-WRW4 for 30 min in PBS containing 0.02% sodium azide. The unbound biotin-WRW4 is washed extensively with PBS containing 0.2% BSA and 0.02% sodium azide. Then the cells are incubated with 5 μg/ml streptavidin-FITC at 4°C for 40 min in the dark. Subsequently, cells are washed twice in washing solution and fixed with 0.2% paraformaldehyde. Fixed cells are analyzed in single laser for FITC with FACSCalibur.

Animal Study:^{^[2]}

Animal Models
male Swiss mice
Dosages
10 μg/paw
Administration
Intraplantar injection

References

Selleck's WRW4 has been cited by 2 publications

Serum amyloid A contributes to radiation-induced lung injury by activating macrophages through FPR2/Rac1/NF-κB pathway [ Int J Biol Sci, 2024, 20(12):4941-4956]	PubMed: 39309438
The analgesic effects of Yu-Xue-Bi tablet (YXB) on mice with inflammatory pain by regulating LXA4-FPR2-TRPA1 pathway [ Chin Med, 2024, 19(1):104]	PubMed: 39107849

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.