MrgprX2 antagonist-10
Based on 1 Customer Validation
MrgprX2 antagonist-10 is a potent MRGPRX2 antagonist. MrgprX2 antagonist-10 inhibits MRGPRX2-mediated accumulation and mast cell degranulation (IC50 < 100 nM), thereby blocking mast cell activation. MrgprX2 antagonist-10 can be used in research on MRGPRX2-related inflammatory and allergic diseases.
For research use only. We do not sell to patients.
- Purity: 98.98%
- CAS No.: 3116848-78-0
- Formula: C26H26F2N8O3
- Molecular Weight:536.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Biological Activity
MrgprX2 antagonist-10 (Example 218) (15 min pre-incubation + 60 min stimulation) shows inhibitory activity against IP1 accumulation in hMRGPRX2-overexpressing HEK293 cells, with an activity grade of "+++" (IC50 < 100 nM)[1].
MrgprX2 antagonist-10 (15 min pre-incubation + 30 min stimulation) shows inhibitory activity against β-hexosamine release in LAD2 human mast cells, with an activity grade of "+++" (IC50 < 100 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3116848-78-0
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Appearance Solid
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Molecular Weight 536.53
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Formula C26H26F2N8O3
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Color Off-white to light yellow
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SMILES
O=C(N1C(C)(CN(CC1)[C@@H](C)C(NC2=NC=C(OC3=C(C=C(C=C3)F)F)N=C2)=O)C)C4=CC5=NC=NN5C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (186.38 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. 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. 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: ≥ 5 mg/mL (9.32 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.32 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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. 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 |
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| DMSO | 1 mM | 1.8638 mL | 9.3191 mL | 18.6383 mL | 46.5957 mL |
| 5 mM | 0.3728 mL | 1.8638 mL | 3.7277 mL | 9.3191 mL | |
| 10 mM | 0.1864 mL | 0.9319 mL | 1.8638 mL | 4.6596 mL | |
| 15 mM | 0.1243 mL | 0.6213 mL | 1.2426 mL | 3.1064 mL | |
| 20 mM | 0.0932 mL | 0.4660 mL | 0.9319 mL | 2.3298 mL | |
| 25 mM | 0.0746 mL | 0.3728 mL | 0.7455 mL | 1.8638 mL | |
| 30 mM | 0.0621 mL | 0.3106 mL | 0.6213 mL | 1.5532 mL | |
| 40 mM | 0.0466 mL | 0.2330 mL | 0.4660 mL | 1.1649 mL | |
| 50 mM | 0.0373 mL | 0.1864 mL | 0.3728 mL | 0.9319 mL | |
| 60 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7766 mL | |
| 80 mM | 0.0233 mL | 0.1165 mL | 0.2330 mL | 0.5824 mL | |
| 100 mM | 0.0186 mL | 0.0932 mL | 0.1864 mL | 0.4660 mL |
MrgprX2 antagonist-10 Related Classifications
HY-185402 Related Classifications
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