Art. -Nr.: HY-107409

GNE 5729

Name: GNE 5729
Brand: MedChemExpress
SKU: HY-107409
Price: 780.00 USD
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GNE 5729 is an orally active, blood-brain barrier-penetrant positive allosteric modulator of NMDARs containing the GluN2A subunit. GNE 5729 enhances NMDAR responses through allosteric modulation, exhibits selectivity over other NMDAR subtypes and AMPARs, and can be used for research on depression.

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Reinheit : 99.05%
CAS. Nr.: 2026635-66-3
Formel: C₁₇H₁₀Cl₂F₃N₅O
Molecular Weight:428.20

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNE 5729 Chemical Structure

CAS. Nr.: 2026635-66-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

NMDA Receptor

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Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.037 μM Compound: 13	Positive allosteric modulation of GluN1/GluN2A receptor (unknown origin) expressed in CHO cells assessed as increase in glutamate-induced calcium flux measured at time interval of 5 mins in presence of saturating glycine by calcium dye-based fluorescence Positive allosteric modulation of GluN1/GluN2A receptor (unknown origin) expressed in CHO cells assessed as increase in glutamate-induced calcium flux measured at time interval of 5 mins in presence of saturating glycine by calcium dye-based fluorescence	[PMID: 28105280]

In Vitro

GNE 5729 (compound 13) is a potent GluN2A PAM with an EC₅₀ of 0.037 μM and a maximum enhancement of 136%, showing over 1000-fold selectivity for NMDAR over AMPAR in NMDAR/AMPAR cellular assays^[1].
GNE 5729 exhibits low human liver microsomal clearance (2 mL/min/kg), an MDCK-MDR1 efflux ratio of 1.6, and a kinetic solubility of 43.5 μM^[1].
GNE 5729 is a moderate inactivator with a tau of 3164 ms and a maximum enhancement of 136% in whole-cell voltage-clamp recordings^[1].
GNE-5729 shows reduced affinity for GluN2A (EC₅₀ = 37 nM) and reduced selectivity for GluN2C and GluN2D (127-fold and 256-fold, respectively) compared with earlier compounds^[4].

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

Parmacokinetics

Species	Dose	Route	CL_blood	T_1/2	V_ss	F
Mice^[1]	0.5 mg/kg	i.v.	10 mL/min/kg	8 h	7 L/kg	/
Mice^[1]	5 mg/kg	p.o.	/	/	/	37 %

Chemical Information

CAS. Nr. 2026635-66-3
Appearance Solid
Molecular Weight 428.20
Formel C₁₇H₁₀Cl₂F₃N₅O
Color White to yellow
SMILES

ClC1=C([C@H]2[C@H](C#N)C2)N3C(C=C1)=NC(CN4N=C(C(F)(F)F)C=C4Cl)=CC3=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (233.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3354 mL

11.6768 mL

23.3536 mL

5 mM

0.4671 mL

2.3354 mL

4.6707 mL

10 mM

0.2335 mL

1.1677 mL

2.3354 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (5.84 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.84 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Villemure E, et al. GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved Profile. ACS medicinal chemistry letters. 2017 Jan 12;8(1):84-89. [Content Brief]

[2]. Wang G, et al. GluN2A: A Promising Target for Developing Novel Antidepressants. The international journal of neuropsychopharmacology. 2024 Sep 01;27(9):pyae037.

[3]. Hanson JE, et al. GluN2A NMDA Receptor Enhancement Improves Brain Oscillations, Synchrony, and Cognitive Functions in Dravet Syndrome and Alzheimer's Disease Models. Cell reports. 2020 Jan 14;30(2):381-396.e4.

[4]. Fu H, et al. Positron Emission Tomography (PET) Ligand Development for Ionotropic Glutamate Receptors: Challenges and Opportunities for Radiotracer Targeting N-Methyl-d-aspartate (NMDA), α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA), and Kainate Receptors. Journal of medicinal chemistry. 2019 Jan 24;62(2):403-419.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.3354 mL	11.6768 mL	23.3536 mL	58.3839 mL
	5 mM	0.4671 mL	2.3354 mL	4.6707 mL	11.6768 mL
	10 mM	0.2335 mL	1.1677 mL	2.3354 mL	5.8384 mL
	15 mM	0.1557 mL	0.7785 mL	1.5569 mL	3.8923 mL
	20 mM	0.1168 mL	0.5838 mL	1.1677 mL	2.9192 mL
	25 mM	0.0934 mL	0.4671 mL	0.9341 mL	2.3354 mL
	30 mM	0.0778 mL	0.3892 mL	0.7785 mL	1.9461 mL
	40 mM	0.0584 mL	0.2919 mL	0.5838 mL	1.4596 mL
	50 mM	0.0467 mL	0.2335 mL	0.4671 mL	1.1677 mL
	60 mM	0.0389 mL	0.1946 mL	0.3892 mL	0.9731 mL
	80 mM	0.0292 mL	0.1460 mL	0.2919 mL	0.7298 mL
	100 mM	0.0234 mL	0.1168 mL	0.2335 mL	0.5838 mL

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GNE 5729

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