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WRW4 FPR antagonist

Name: WRW4
Brand: Selleck Chemicals
SKU: S9818
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S9818

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

Chemical Structure

Molecular Weight: 1104.27

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.53

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other FPR Inhibitors	HCH6-1 N-Formyl-Met-Leu-Phe (fMLP) FPR Agonist 43 BMS-986235

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (90.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 50 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (4.53mM)	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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (0.72mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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 ddH₂O, 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.

Chemical Information, Storage & Stability

Molecular Weight	1104.27	Formula	C₆₁H₆₅N₁₅O₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	878557-55-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	FPRL1 (Cell-free assay) 0.23 μM
In vitro	WRW4 shows potent activity in terms of inhibiting WKYMVm binding to FPRL1. It 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. This compound 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 this chemical, which also completely inhibits the internalization of Aβ42 peptide in human macrophages.
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 this compound prevents the increase of ANXA1 levels induced by EA.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15210823/ [2] https://pubmed.ncbi.nlm.nih.gov/33474635/

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