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NP10679

CAT: 0804-HY-148825-01Size: 10 mM - 1 mLDry Ice: NoHazardous: No
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CAT#:0804-HY-148825-01Size:10 mM - 1 mL
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
H1 Receptor; α adrenergic receptor

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