1. GPCR/G Protein
  2. Mas-related G-protein-coupled Receptor (MRGPR)
  3. MrgprX2 antagonist-1

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.

MrgprX2 antagonist-1 Chemical Structure

MrgprX2 antagonist-1 Chemical Structure

CAS No. : 2642162-06-7

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1 mg USD 140 In-stock
5 mg USD 350 In-stock
10 mg USD 600 In-stock
25 mg USD 1250 In-stock
50 mg USD 1950 In-stock
100 mg USD 3200 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE MrgprX2 antagonist-1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

MrgprX2[1]

In Vitro

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.

Molecular Weight

410.36

Formula

C15H15F5N4O2S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

FC(F)(F)[C@H](O)CN(CC)C(NC1=NN=C(S1)CC2=CC(F)=CC(F)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4369 mL 12.1844 mL 24.3688 mL
5 mM 0.4874 mL 2.4369 mL 4.8738 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MrgprX2 antagonist-1
Cat. No.:
HY-145191
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