WRW4

Catalog No.S9818 Batch:S981801

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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)
 
* <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

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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.