Home GPCR & G Protein FPR antagonist WRW4 For research use only.

WRW4

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).

WRW4 Chemical Structure

WRW4 Chemical Structure

CAS No. 878557-55-2

Purity & Quality Control

Batch: S981801 DMSO]100 mg/mL]false]Water]50 mg/mL]false]]]false Purity: 99.53%
99.53

WRW4 Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models male Swiss mice
Dosages 10 μg/paw
Administration Intraplantar injection

Chemical Information & Solubility

Molecular Weight 1104.27 Formula

C61H65N15O6
CAS No. 878557-55-2 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (90.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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