NP10679

SKU: orb1744162

Description

NP10679 is a potent, brain-penetrant, and pH-sensitive GluN2B-selective NMDA receptor antagonist with oral bioavailability. Its off-target activity includes inhibition of histamine H1 and hERG. This profile makes it a useful research tool for investigating mechanisms in epilepsy and ischemic stroke models, both in vitro and in vivo.

Research Area

Immunology & Inflammation, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2914889-88-4
• MW: 449.47
• Purity: 99.43%
• Formula: C₂₃H₂₆F₃N₃O₃
• SMILES: O(C[C@@H](CN1CCN(CC1)C2=CC=C(C(F)(F)F)C=C2)O)C=3C=C4C(=CC3)NC(=O)CC4
• Target: Cytochromes P450,Potassium Channel,NMDAR,Histamine Receptor
• Solubility: DMSO:80 mg/mL (177.99 mM)

Bioactivity

• Target IC50:
  α1B-adrenoceptor:1.92 μM (Ki)|α1D-adrenoceptor:0.495 μM (Ki)|α2C-adrenoceptor:3.09 μM (Ki)|α1A-adrenoceptor:0.154 μM|α1A-adrenoceptor:0.603 μM (Ki)|H1 Receptor:0.073 μM|H1 Receptor:0.04 μM (Ki)
• In Vivo:
  In the Male C57BL/6 middle cerebral artery occlusion (MCAo) model of transient ischemia mice, NP10679 (2, 5, and 10 mg/kg; intraperitoneal injection; administered 15 minutes prior to transient ischemia) dose-dependently reduces infarct volumes, with an ED50 of 1 mg/kg.
• In Vitro:
  NP10679 is an NMDA receptor inhibitor containing GluN2B that is more effective than physiological pH. It exhibits inhibitory effects on 5-HT2A, α1A adrenergic receptor, H1 histamine receptor, and hERG channels.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NMDA receptor, Histamine Receptor, HistamineReceptor, hERG, CYP

Compound Identifiers

PubChem CID

162623707