NMDA receptor antagonist 4 NEW
| Price | Get Latest Price | ||
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-07-22 |
Product Details
| Product Name: NMDA receptor antagonist 4 | CAS No.: 1607589-56-9 |
| Supply Ability: 10g | Release date: 2025/07/22 |
Product Introduction
Bioactivity
| Name | NMDA receptor antagonist 4 |
| Description | NMDA receptor antagonist 4 (IIc) is an uncompetitive, voltage-dependent, orally active NMDAR blocker with an IC50 of 1.93 μM. It shows positive predicted blood-brain-barrier (BBB) permeability and can be used in Alzheimer's disease research[1]. |
| In vitro | NMDA receptor antagonist 4 (IIc) competitively interacts with the endogenous blocker Mg2+ and exhibits membrane potential dependence in the NMDAR channel [1]. It shows high metabolic stability in human and mouse liver microsomes and demonstrates hERG safety without observable cytotoxicity [1]. In a cell cytotoxicity assay using Neuro2A cells, at concentrations of 1, 10, and 100 μM over 24 hours, it did not show cytotoxicity at the highest concentration tested (100 μM) [1]. |
| In vivo | NMDA receptor antagonist 4 (IIc) exhibited significant neuroprotective effects in vitro and in vivo at 0-10 μM, reducing motor deficits and protecting against Aβ toxin-induced neuronal dysfunction. Orally administered at 5 mg/kg/day for four weeks, it enhanced cell survival and synaptic function in Alzheimer's disease models, attributed to activation of the Fyn-GluN2B-CREB signaling pathway and prevention of synaptic NMDARs internalization. In C. elegans models (N2 wild-type, CL2006, CL2122, CL2355), it ameliorated defective locomotion in CL2006 nematodes and improved chemotaxis in CL2355 nematodes affected by Aβ expression. In six-month-old female 5XFAD mice, the treatment regimen enhanced working memory function, restored GluN2A and postsynaptic density protein (PSD) 95 expression, increased Fyn and GluN2B phosphorylation, significantly raised p-CREB protein levels in the nucleus, and reverted calbindin D-28K protein levels. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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