MrgprX2 antagonist-1
Based on 5 publication(s) in Google Scholar
MrgprX2 antagonist-1 is an MrgprX2 antagonist extracted from patent WO2021092264A1, example E23. MrgprX2 antagonist-1 can be used for the research of inflammatory disorders of the skin.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 2642162-06-7
- Formula: C15H15F5N4O2S
- Molecular Weight:410.36
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MrgprX2 antagonist-1
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Customer Validation & Images
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Histological Imaging/Staining
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ELISA
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IF
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IHC
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IF
Biological Activity
MrgprX2[1]
MRGPRX2, a member of the Mas-related gene family, was found to be expressed in sensory neurons, mast cells and, most recently, in keratinocytes. MRGPRX2 mRNA is present in adipose tissue, esophagus, urinary bladder, lungs with the highest levels found in skin. Activation of MRGPRX2 leads to mast cell degranulation with subsequent pseudo-allergic reactions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2642162-06-7
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Appearance Solid
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Molecular Weight 410.36
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Formula C15H15F5N4O2S
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Color White to light yellow
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SMILES
FC(F)(F)[C@H](O)CN(CC)C(NC1=NN=C(S1)CC2=CC(F)=CC(F)=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Allergy
Meglumine gadoterate induces immunoglobulin-independent human mast cell activation via MRGPRX2. [Abstract]2023 Dec;78(12):3255-3258. PMID: 37548384 -
J Invest Dermatol
MRGPRX2-Mediated Mast Cell Activation Promotes Malignant Progression of Cutaneous Squamous Cell Carcinoma through IL-17A Release. [Abstract]2025 Nov 4:S0022-202X(25)03517-1. PMID: 41197765 -
Inflammopharmacology
Casticin reduces rosacea-related inflammation by inhibiting mast cell activation via Mas-related G protein-coupled receptor X2. [Abstract]2025 Apr;33(4):1935-1947. PMID: 39821787
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Inflammopharmacology. 2025 Apr;33(4):1935-1947. [Abstract]
MrgprX2 antagonist-1(po) in LL‑37‑induced rosacea‑like mouse model reduced epidermal injury and inflammatory cell infiltration compared to the control group.
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Inflammopharmacology. 2025 Apr;33(4):1935-1947. [Abstract]
MrgprX2 antagonist-1 (12 h) LAD2 cells with 10 μg/ml LL-37 significantly reduced TPS, TNF-α, MMP-9, and IL-1β protein levels.
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Inflammopharmacology. 2025 Apr;33(4):1935-1947. [Abstract]
MrgprX2 antagonist-1 (po) in LL‑37‑induced rosacea‑like mouse model inhibited MC activation in rosacea lesions and the MC response was significantly reduced.
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Inflammopharmacology. 2025 Apr;33(4):1935-1947. [Abstract]
MrgprX2 antagonist-1 (po) in LL‑37‑induced rosacea‑like mouse model significantly reduced CD4+ T cell infiltration.
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Eur J Pharmacol
Systemic administration of Neochamaejasmin B inhibits mast cell activation to reduce inflammation in a rosacea mouse model by targeting MRGPRX2. [Abstract]2025 Sep 15:1003:177988. PMID: 40706973 -
Immunopharmacol Immunotoxicol
Evaluation of the inhibitory effect of different molecular weights chitosan on MRGPRX2-mediated mast cell degranulation and the pseudo-allergic reaction. [Abstract]2025 Jan 22:1-11. PMID: 39842105
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Immunopharmacol Immunotoxicol. 2025 Jan 22:1-11. [Abstract]
MrgprX2 antagonist-1 (5 mg/kg；po) reduced mast cell activation in the LL-37-induced rosacea mouse model in C57BL/6 mice.
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Immunopharmacol Immunotoxicol. 2025 Jan 22:1-11. [Abstract]
MrgprX2 antagonist-1 (5 mg/kg；po) reduced CD4+T cells infiltration in LL-37-induced rosacea mouse model in C57BL/6 mice.
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Immunopharmacol Immunotoxicol. 2025 Jan 22:1-11. [Abstract]
MrgprX2 antagonist-1 (5 mg/kg；po) reduced TPS, TNF-α, IL-1β and MMP-9 concentration in the skin lesion of LL-37-induced rosacea mouse model.
MrgprX2 antagonist-1 purchased from MedChemExpress. Usage Cited in: Immunopharmacol Immunotoxicol. 2025 Jan 22:1-11. [Abstract]
MrgprX2 antagonist-1 (5 μg/mL) down-regulated the phosphorylation level of p65 and up-regulated the phosphorylation level of IκB analyzed by western blotting.
Solvent & Solubility
DMSO : 66.67 mg/mL (162.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4369 mL | 12.1844 mL | 24.3688 mL | 60.9221 mL |
| 5 mM | 0.4874 mL | 2.4369 mL | 4.8738 mL | 12.1844 mL | |
| 10 mM | 0.2437 mL | 1.2184 mL | 2.4369 mL | 6.0922 mL | |
| 15 mM | 0.1625 mL | 0.8123 mL | 1.6246 mL | 4.0615 mL | |
| 20 mM | 0.1218 mL | 0.6092 mL | 1.2184 mL | 3.0461 mL | |
| 25 mM | 0.0975 mL | 0.4874 mL | 0.9748 mL | 2.4369 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8123 mL | 2.0307 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6092 mL | 1.5231 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4874 mL | 1.2184 mL | |
| 60 mM | 0.0406 mL | 0.2031 mL | 0.4061 mL | 1.0154 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7615 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6092 mL |
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