QWF |
Catalog No.GC50531
One-Click Copy Product Info
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QWF is a specific antagonist of MRGPRX2 and also an NK1 receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 126088-82-2
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 126088-82-2 | SDF | |
| Canonical 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 | ||
| Formula | C38H43N5O8 | M.Wt | 697.78 |
| Solubility | 10mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4331 mL | 7.1656 mL | 14.3312 mL |
| 5 mM | 286.6 μL | 1.4331 mL | 2.8662 mL |
| 10 mM | 143.3 μL | 716.6 μL | 1.4331 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >96.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)