2. GPCR/G Protein
  3. Mas-related G-protein-coupled Receptor (MRGPR)
  4. ML382

ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.

For research use only. We do not sell to patients.

ML382 Chemical Structure

ML382 Chemical Structure

CAS No. : 1646499-97-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 95 In-stock
Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Solid
5 mg USD 87 In-stock
10 mg USD 140 In-stock
50 mg USD 480 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ML382 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM[1].

IC50 & Target

EC50: 190 nM (MRGPRX1)[1]
In Vitro

In the absence of ML382, the IC50 for BAM8-22 inhibition of ICa is 0.66 ± 0.05 μM. In the presence of 0.1 μM, 1 μM, 10 μM, and 30 μM ML382, BAM8-22 IC50 is reduced to 0.43 ± 0.02 μM, 0.25 ± 0.02 μM, 0.06 ± 0.01 μM, and 0.08 ± 0.01 μM, respectively. A lower IC50 generally indicates a higher potency; thus, ML382 dose-dependently increases the potency of BAM8–22, further demonstrating that ML382 is a positive allosteric modulator of MRGPRX1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ML382 Related Antibodies
In Vivo

ML382 (5 μM) significantly increases inhibition of ICa by a low concentration of BAM8–22 (0.5 μM) in DRG neurons from MrgprX1 mice. ML382 enhances the inhibition of spinal synaptic transmission by BAM8-22 in MrgprX1 mice. ML382 (25 μM, 125 μM, and 250 μM; 5 μL; i.th.;) dose-dependently attenuates heat hypersensitivity in MrgprX1 mice. ML382 (lumbar puncture injection; 25 μM, 5 μL) leads to a significant increase in postconditioning time spent in the ML382-paired chamber, compared with the preconditioning value. ML382 inhibits nerve injury-induced ongoing pain in MrgprX1 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

360.43

Formula

C18H20N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC=C1OCC)C2=CC=CC=C2NS(=O)(C3CC3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (277.45 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 2.7745 mL 13.8723 mL 27.7446 mL
5 mM 0.5549 mL 2.7745 mL 5.5489 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. 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 (6.94 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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. 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 2.7745 mL 13.8723 mL 27.7446 mL 69.3616 mL
5 mM 0.5549 mL 2.7745 mL 5.5489 mL 13.8723 mL
10 mM 0.2774 mL 1.3872 mL 2.7745 mL 6.9362 mL
15 mM 0.1850 mL 0.9248 mL 1.8496 mL 4.6241 mL
20 mM 0.1387 mL 0.6936 mL 1.3872 mL 3.4681 mL
25 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7745 mL
30 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3121 mL
40 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7340 mL
50 mM 0.0555 mL 0.2774 mL 0.5549 mL 1.3872 mL
60 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8670 mL
100 mM 0.0277 mL 0.1387 mL 0.2774 mL 0.6936 mL
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ML382 Related Classifications

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.

Keywords:

ML3821646499-97-9ML 382ML-382Mas-related G-protein-coupled Receptor (MRGPR)painnociceptornervousDRGneuronsinjuryInhibitorinhibitorinhibit

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