NP10679

NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes[1].

Product Specifications

CAS Number

[2914889-88-4]

UNSPSC

12352005

Target

Adrenergic Receptor; Cytochrome P450; Histamine Receptor; iGluR; Potassium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Cancer; Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/np10679.html

Concentration

10mM

Purity

98.40

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1)CCC2=C1C=CC(OC[C@H](O)CN(CC3)CCN3C4=CC=C(C(F)(F)F)C=C4)=C2

Molecular Formula

C23H26F3N3O3

Molecular Weight

449.47

References & Citations

[1]Zaczek R, et al. Phase 1 Clinical Results for NP10679, a pH-sensitive GluN2B-selective N-methyl-d-aspartate Receptor Inhibitor. Clin Pharmacol Drug Dev. 2023 Jan 15.|[2]Myers SJ, et al. A Glutamate N-Methyl-d-Aspartate (NMDA) Receptor Subunit 2B-Selective Inhibitor of NMDA Receptor Function with Enhanced Potency at Acidic pH and Oral Bioavailability for Clinical Use. J Pharmacol Exp Ther. 2021 Oct;379 (1) :41-52.