NMDAR antagonist 1

Name: NMDAR antagonist 1
Brand: MedChemExpress
SKU: HY-111500A
Rating: 4.5 (1 reviews)

Cat. No.: HY-111500A Purity: 99.02%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.

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

NMDAR antagonist 1 Chemical Structure

CAS No. : 2220162-06-9

Size	Price	Stock	Quantity
5 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	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

Other Forms of NMDAR antagonist 1:

(Rac)-NMDAR antagonist 1 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist^[1].

IC₅₀ & Target

NMDAR^[1]

In Vitro

NMDAR antagonist 1 (Compound 5q) exhibits excellent neuroprotective activity^[1].
NMDAR antagonist 1 can attenuate Ca²⁺ influx induced by NMDA^[1].
NMDAR antagonist 1 can suppress the NR2B up-regulation and increase p-ERK1/2 expression^[1].
NMDAR antagonist 1 inhibits SH-SY5Y cells with cell viabilities of 75.8%, 80.0%, 84.4%, and 78.6% at 0.1 µM 1 µM 10 µM 100 µM, respectively^[1].

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

Molecular Weight

414.30

Formula

C₂₀H₂₀BrN₃O₂

CAS No.

2220162-06-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCC1=CC=C(O)C=C1)[C@@H]2CCC3=NC4=CC=C(Br)C=C4CN32

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 : 6.67 mg/mL (16.10 mM; ultrasonic and warming and heat to 60°C; 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	2.4137 mL	12.0685 mL	24.1371 mL
5 mM	0.4827 mL	2.4137 mL	4.8274 mL
10 mM	0.2414 mL	1.2069 mL	2.4137 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: ≥ 0.67 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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: ≥ 0.67 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 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 (6.7 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)

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: 99.02%

Select Batch:

Data Sheet (270 KB) SDS (393 KB)

COA (247 KB) HNMR (113 KB) RP-HPLC (153 KB) LCMS (200 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang L, et al. Design, synthesis and bioevaluation of 1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline-1-carboxylic acid derivatives as potent neuroprotective agents. Eur J Med Chem. 2018 May 10;151:27-38. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4137 mL	12.0685 mL	24.1371 mL	60.3427 mL
	5 mM	0.4827 mL	2.4137 mL	4.8274 mL	12.0685 mL
	10 mM	0.2414 mL	1.2069 mL	2.4137 mL	6.0343 mL
	15 mM	0.1609 mL	0.8046 mL	1.6091 mL	4.0228 mL