GLPBio

QWF

Catalog No.: GC50531Purity:>96.00%
COASDSData Sheet
QWF is a specific antagonist of MRGPRX2 and also an NK1 receptor antagonist.

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QWF
Cas No.: 126088-82-2
5mgIn Stock
$323.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

Beschreibung (Description)

QWF is a specific antagonist of MRGPRX2 and also an NK1 receptor antagonist[1]. Mas-related G protein-coupled receptor X2 (MRGPRX2) is a receptor expressed primarily on mast cells and sensory neurons, playing an important role in mediating itch and pain sensations[2]. QWF is usually used in research on pain, inflammation, and allergic reactions[3][4].

In vitro, pre-incubation of HMC1 mast cells with QWF (10, 25, and 100mM; 10min) dose-dependently inhibited C48/80-induced degranulation, and significantly suppressed CD63 surface membrane expression and β-hexosaminidase release[5].

In vivo, QWF (20mg/kg/day; i.p.; beginning in the 7th week after surgery for 2 weeks) reversed endometriosis-induced mechanical and thermal hyperalgesia and reduced ectopic lesion volume and weight in wild-type C57BL/6J mice[6]. QWF (500μM; 10μL; intradermal injection) co-administered with lithocholic acid (LCA) reduced the LCA-induced scratching behavior in ICR mice[7].

References:
[1] Hagiwara D, Miyake H, Morimoto H, Murai M, Fujii T, Matsuo M. Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists. J Med Chem. 1992;35(11):2015-2025.
[2] Kuhn H, Kolkhir P, Babina M, et al. Mas-related G protein-coupled receptor X2 and its activators in dermatologic allergies. J Allergy Clin Immunol. 2021;147(2):456-469.
[3] Azimi E, Reddy VB, Shade KC, et al. Dual action of neurokinin-1 antagonists on Mas-related GPCRs. JCI Insight. 2016;1(16):e89362.
[4] Iio K, Kutsumura N, Nagumo Y, et al. Synthesis of unnatural morphinan compounds to induce itch-like behaviors in mice: Towards the development of MRGPRX2 selective ligands. Bioorg Med Chem Lett. 2022;56:128485.
[5] Hermans MAW, van Stigt AC, van de Meerendonk S, et al. Human Mast Cell Line HMC1 Expresses Functional Mas-Related G-Protein Coupled Receptor 2. Front Immunol. 2021;12:625284.
[6] Mao X, Wang J, Ding S, et al. MRGPRX2 Mediates Mast Cell-Induced Endometriosis Pain Through the Sensitization of Sensory Neurons via Histamine/HRH1/TRPV1 Signaling Pathway. FASEB J. 2025;39(13):e70778.
[7] Song MH, Shim WS. Lithocholic Acid Activates Mas-Related G Protein-Coupled Receptors, Contributing to Itch in Mice. Biomol Ther (Seoul). 2022;30(1):38-47.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

HMC1 mast cells

Preparation Method

HMC1 cells were cultured in Roswell Park Memorial Institute medium supplemented with HEPES, 10% inactivated fetal calf serum (FCS), 50μM β‐mercapto‐ethanol, and 1% antibiotics (penicillin/streptomycin). Stimulation experiments were performed using the MRGPRX2 specific ligand compound 48/80 (1-100mg/ml). To further prove the functionality and specificity of MRGPRX2 activation, additional inhibition experiments were conducted by pre-incubation with the MRGPRX2 specific antagonist QWF for 10 minutes, at concentrations of 10, 25 and 100mM. An unstimulated condition containing an equal amount of the QWF diluent, dimethyl sulfoxide (DMSO), was included in every experiment as a control condition, not exceeding the maximal concentration of 0.28% DMSO during stimulation of the cells. Degranulation was assessed by β-hexosaminidase release and CD63 expression.

Reaction Conditions

10, 25, and 100mM; 10min

Applications

Pre-incubation of HMC1 mast cells with QWF dose-dependently inhibited C48/80-induced degranulation, and significantly suppressed CD63 surface membrane expression and β-hexosaminidase release.
Animal experiment [2]:

Animal models

female C57BL/6J wild-type mice

Preparation Method

Six to eight-week-old female C57BL/6J wild-type control mice were housed under identical conditions, with a maximum of 5 animals per cage, on a 12-hour light–dark cycle. Food and water were provided ad libitum. Endometriosis was induced as follows: bilateral ovariectomy was performed seven days before the operation, followed by subcutaneous injection of 0.5mg of oestradiol benzoate dissolved in 60mL of corn oil every 5 days. On Day 0, the uterine tissue of each donor was dissected and cut into fragments less than 1mm3 in size. These fragments were then suspended in 0.9% sterile saline and injected intraperitoneally into two other recipient mice. The Sham operation group received an equivalent volume of 0.9% sterile saline. WT mice were separated into three groups to investigate the role of Mrgprb2 in endometriosis-induced hyperalgesia: the Sham group, drug groups, and the control group. The mice in the Sham and control groups were injected intraperitoneally with the vehicle control containing 10% DMSO, 40% PEG400, 5% Tween-80 and 45% saline, while those in the drug administration group were injected with the Mrgprb2 antagonist QWF (i.p.) at a dose of 20mg/kg once a day. Behavioral tests, including mechanical and thermal paw withdrawal tests and reflexive withdrawal tests to mechanical and thermal stimulation of the abdominal area, were performed to assess hyperalgesia in the mice before and every week after surgery. The mice were anesthetized via the inhalation of CO2 and euthanized via cervical dislocation on Days 28 or 49 after the induction of endometriosis. The peritoneal fluid and DRG (T11-L2 segment) were preserved for further experiments.

Dosage form

20mg/kg/day; i.p. beginning in the 7th week after surgery for 2 weeks

Applications

QWF reversed endometriosis-induced mechanical and thermal hyperalgesia and reduced ectopic lesion volume and weight in wild-type C57BL/6J mice.

References:
[1] Hermans MAW, van Stigt AC, van de Meerendonk S, et al. Human Mast Cell Line HMC1 Expresses Functional Mas-Related G-Protein Coupled Receptor 2. Front Immunol. 2021;12:625284.
[2] Mao X, Wang J, Ding S, et al. MRGPRX2 Mediates Mast Cell-Induced Endometriosis Pain Through the Sensitization of Sensory Neurons via Histamine/HRH1/TRPV1 Signaling Pathway. FASEB J. 2025;39(13):e70778.

Produktdokumente (Product Documents)

Purity:>96.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
126088-82-2
SMILES
CC(C)(C)OC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CC1=CN(C=O)C2=CC=CC=C12)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)OCC1=CC=CC=C1
Summenformel
C38H43N5O8
Molekulargewicht
697.78
Löslichkeit
10mg/mL in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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