QWF
目录号 : GC50531QWF是一种特异性的MRGPRX2拮抗剂，同时也是NK1受体拮抗剂。
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.
QWF是一种特异性的MRGPRX2拮抗剂，同时也是NK1受体拮抗剂[1]。Mas-related G protein-coupled receptor X2（MRGPRX2）是一种主要在肥大细胞和感觉神经元上表达的受体，在介导瘙痒和疼痛感觉中起关键作用[2]。QWF通常用于疼痛、炎症和过敏反应的研究[3][4]。
体外实验中，用QWF（10、25和100mM）预孵育HMC1肥大细胞10分钟，可剂量依赖性地抑制C48/80诱导的脱颗粒，并显著抑制CD63表面膜表达和β-己糖胺酶的释放[5]。
体内实验中，QWF（20mg/kg/天；腹腔注射；从手术后第7周开始，连续2周）可逆转野生型C57BL/6J小鼠子宫内膜异位症引起的机械性超敏和热超敏反应，并减少异位病灶的体积和重量[6]。QWF （500μM；10μL；皮内注射）与石胆酸（LCA）共给药可减少LCA诱导的ICR小鼠抓挠行为[7]。
| 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 | ||
| 分子式 | C38H43N5O8 | 分子量 | 697.78 |
| 溶解度 | 10mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >96.00%
- COA (Certificate Of Analysis)
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