2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. ML254

ML254 is a potent mGlu5 potentiator, with EC50 and pEC50 of 9.3 nM and 8.03 nM for rat mGlu5, respectively. ML254 can be used for researching schizophrenia. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

ML254 Chemical Structure

ML254 Chemical Structure

CAS No. : 1428630-86-7

Size Price Stock Quantity
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
50 mg USD 850 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

ML254 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ML254 is a potent mGlu5 potentiator, with EC50 and pEC50 of 9.3 nM and 8.03 nM for rat mGlu5, respectively. ML254 can be used for researching schizophrenia[1]. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

rat mGluR5

9.3 nM (EC50)

rat mGluR5

8.03 nM (pEC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
9.3 nM
Compound: 38t, VU0430644, ML254
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4AM dye-based fluorescence assay
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4AM dye-based fluorescence assay
[PMID: 24050755]
Molecular Weight

310.32

Formula

C18H15FN2O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1(C)COC1)C2=NC=C(C#CC3=CC=CC(F)=C3)C=C2
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 (322.25 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 3.2225 mL 16.1124 mL 32.2248 mL
5 mM 0.6445 mL 3.2225 mL 6.4450 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
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Volume
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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 (8.06 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.
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 3.2225 mL 16.1124 mL 32.2248 mL 80.5620 mL
5 mM 0.6445 mL 3.2225 mL 6.4450 mL 16.1124 mL
10 mM 0.3222 mL 1.6112 mL 3.2225 mL 8.0562 mL
15 mM 0.2148 mL 1.0742 mL 2.1483 mL 5.3708 mL
20 mM 0.1611 mL 0.8056 mL 1.6112 mL 4.0281 mL
25 mM 0.1289 mL 0.6445 mL 1.2890 mL 3.2225 mL
30 mM 0.1074 mL 0.5371 mL 1.0742 mL 2.6854 mL
40 mM 0.0806 mL 0.4028 mL 0.8056 mL 2.0140 mL
50 mM 0.0644 mL 0.3222 mL 0.6445 mL 1.6112 mL
60 mM 0.0537 mL 0.2685 mL 0.5371 mL 1.3427 mL
80 mM 0.0403 mL 0.2014 mL 0.4028 mL 1.0070 mL
100 mM 0.0322 mL 0.1611 mL 0.3222 mL 0.8056 mL
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ML254 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:

ML2541428630-86-7ML 254ML-254mGluRMetabotropic glutamate receptorsSchizophreniaInhibitorinhibitorinhibit

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