2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. GNE-9278

GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.

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GNE-9278 Chemical Structure

GNE-9278 Chemical Structure

CAS No. : 2315311-83-0

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Based on 1 publication(s) in Google Scholar

GNE-9278 Related Antibodies

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Description

GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity[1].

IC50 & Target

NMDAR[1]
In Vitro

GNE-9278 (50 μM) slows deactivation with multiple agonists (D-Glu, L-Glu and L-CCG-IV) and enhances the potency of both Glu and Gly[1].
GNE-9278 robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs as measured by calcium influx assays from HEK cell lines with EC50s of 0.74, 3.07, 0.47, and 0.32 μM, respectively[1].

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

GNE-9278 Related Antibodies
Molecular Weight

429.54

Formula

C21H27N5O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(N=C2CCC)C(N2)=NC(C)=C1N[S](=O)(C3=CC=C(C4CCCCC4)C=C3)=O
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 : 2 mg/mL (4.66 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 2.3281 mL 11.6404 mL 23.2807 mL
5 mM --- --- ---
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.

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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 2.3281 mL 11.6404 mL 23.2807 mL 58.2018 mL
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GNE-9278 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:

GNE-92782315311-83-0GNE9278GNE 9278iGluRIonotropic glutamate receptorspositiveallostericNMDARGluN1transmembranedomainTMDcurrentagonistaffinityInhibitorinhibitorinhibit

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