GNE-5729 | CAS 2026635-66-3

GNE-5729

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Cat #: V2130 CAS #: 2026635-66-3 Purity ≥ 98%

Description: GNE 5729 is a novel, potent, brain permeable positive allosteric modulator (PAM) and GluN2A subunit-selective of NMDAR with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively. The N-methyl-d-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, gated by the endogenous coagonists glutamate and glycine, permeable to Ca2+ and Na+. NMDAR dysfunction is associated with numerous neurological and psychiatric disorders, including schizophrenia, depression, and Alzheimer's disease. GNE-0723 is a and brain-penetrant positive allosteric modulatorof NMDARs.

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CAS No.	2026635-66-3
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent

Related Biological Data

(A) Overlay of modeled compound 3 (purple) and GluN2A/GluN1 X-ray cocrystal structure with compound 2 (PDB ID 5TP9 gray). The amide in compound 3 may force the larger core to clash slightly with Glu132. Distances are between the Glu132 backbone nitrogen and hydrogen in 3 or sulfur in 2. (B) Overlay of a model of compound 3 (purple) and X-ray crystal structure of compound 9 (PDB ID 5TPA, gray). The cyclopropyl nitrile in 9 may allow the larger core to shift away from Glu132. Distances are between the Glu132 backbone nitrogen and hydrogens in 3 and 9. ACS Med Chem Lett. 2017 Jan 12; 8(1): 84–89.

(A) Overlay of whole cell voltage clamp recordings comparing deactivation kinetics for GNE-0723 (1) in red and GNE-5729 (13) in blue compared to the endogenous coagonists (saturating glycine and 100 μM glutamate) in black. ACS Med Chem Lett. 2017 Jan 12; 8(1): 84–89.

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

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Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

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Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.