mGluR5 antagonist-1

Name: mGluR5 antagonist-1
Brand: MedChemExpress
SKU: HY-155352
Rating: 4.5 (1 reviews)

Cat. No.: HY-155352 Purity: 98.80%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

mGluR5 antagonist-1 (compound 10) is a high-affinity mGluR5 antagonist, with an IC₅₀ value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect.

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

mGluR5 antagonist-1 Chemical Structure

CAS No. : 2761424-76-2

Size	Price	Stock	Quantity
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1120	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

mGluR5 antagonist-1 (compound 10) is a high-affinity mGluR5 antagonist, with an IC₅₀ value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect^[1].

Molecular Weight

382.41

Formula

C₂₃H₁₈N₄O₂

CAS No.

2761424-76-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

CN1C2=NC=NC(C#CC3=CC=CC=C3)=C2C=C1C(NC4=CC=C(OC)C=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (523.00 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	2.6150 mL	13.0750 mL	26.1499 mL
5 mM	0.5230 mL	2.6150 mL	5.2300 mL
10 mM	0.2615 mL	1.3075 mL	2.6150 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 5 mg/mL (13.07 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 98.80%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (251 KB) HNMR (259 KB) RP-HPLC (105 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Yonglei Du, et al. Novel substituted 4-(Arylethynyl)-Pyrrolo[2,3-d]pyrimidines negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGlu5) Treat depressive disorder in mice. Eur J Med Chem. 2023. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6150 mL	13.0750 mL	26.1499 mL	65.3749 mL
	5 mM	0.5230 mL	2.6150 mL	5.2300 mL	13.0750 mL
	10 mM	0.2615 mL	1.3075 mL	2.6150 mL	6.5375 mL
	15 mM	0.1743 mL	0.8717 mL	1.7433 mL	4.3583 mL
	20 mM	0.1307 mL	0.6537 mL	1.3075 mL	3.2687 mL
	25 mM	0.1046 mL	0.5230 mL	1.0460 mL	2.6150 mL
	30 mM	0.0872 mL	0.4358 mL	0.8717 mL	2.1792 mL
	40 mM	0.0654 mL	0.3269 mL	0.6537 mL	1.6344 mL
	50 mM	0.0523 mL	0.2615 mL	0.5230 mL	1.3075 mL
	60 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0896 mL
	80 mM	0.0327 mL	0.1634 mL	0.3269 mL	0.8172 mL
	100 mM	0.0261 mL	0.1307 mL	0.2615 mL	0.6537 mL