SML2603

GNE-9278

≥98% (HPLC)

• Synonym(e): 4-Cyclohexyl-N-(7-hydroxy-5-methyl-2-propyl[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)-benzenesulfonamide, GNE 9278, GNE9278
• Empirische Formel (Hill-System): C₂₁H₂₇N₅O₃S
• CAS-Nummer: 901230-11-3
• Molekulargewicht: 429.54
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CC1=NC2=NC(CCC)=NN2C(O)=C1NS(C3=CC=C(C4CCCCC4)C=C3)(=O)=O

Beschreibung

Biochem/physiol Actions

GNE-9278 is a selective NMDAR, but not AMPAR, positive allosteric modulator (PAM fold enhancement Emax/EC50 = 5.5/0.74 μM/2A, 8.4/3.07 μM/2B,10.2/0.47 μM/2C, 7.9/0.32 μM/2D of gly EC50 (50 μM)-induced Ca++ influx in HEK293 co-expressing GluN1 & respective GluN2 subunit; Emax/EC50 = 4.6/3.2 μM/2A,12.4/15.7 μM/2B, 9.1/6.6 μM/2C, 14.9/6.7 μM/2D of 100 μM Glu-induced current in the presence of 50 μM gly using respective GluN1/GluN2 oocytes). GNE-9278 targets transmembrane domain (TMD) extracellular surface of agonist-bound NMDARs, stabilizing NMDARs in an activated state by slowing L-L-glu & gly off-rate.

Selective NMDAR, but not AMPAR, positive allosteric modulator (PAM) that targets TMD extracellular surface of ligand-bound NMDARs and slows L-Glu/Gly dissociation.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable