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NP10679

$48$923

Products Details

Product Description

– 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].

Web ID

– HY-148825

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Metabolism-sugar/lipid metabolism

Molecular Formula

– C23H26F3N3O3

References

– [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.

CAS Number

– 2914889-88-4

Molecular Weight

– 449.47

Compound Purity

– 99.42

SMILES

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

Clinical Information

– Phase 1

Research Area

– Cancer; Metabolic Disease; Inflammation/Immunology

Solubility

– 10 mM in DMSO

Target

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

Isoform

– H1 Receptor;α adrenergic receptor

Pathway

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

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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