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| Targets |
Nelonemdaz targets N-methyl-D-aspartate (NMDA) receptors, specifically the NR2B subunit, and acts as a free radical scavenger. It is an NR2B-selective and uncompetitive NMDA receptor antagonist. By selectively blocking NR2B-containing NMDA receptors, Nelonemdaz reduces excitotoxicity, a key mechanism of neuronal injury. Additionally, its free radical scavenging activity reduces oxidative stress. This dual mechanism provides neuroprotection against both NMDA- and free radical-induced cell death.
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| ln Vitro |
Nelonemdaz (10-300 μM) exhibits noteworthy neuroprotective properties at dosages as low as 30 μM against 300 μM N-methyl-d-aspartate (NMDA) [1]. In a concentration-dependent manner, nelonemdazl (10-500 μM) suppresses the electrophysiological response of cultured cortical neurons to 300 μM NMDA [1]. Fe2+-induced neurotoxicity can be considerably mitigated by nelonemdaz (0.1–1 μM), even at dosages as low as 0.1–0.3 μM [1]. Nelonemdaz (0.1–1 μM) stops the degradation of neurons and glial cells in cortical cell cultures [1]. It has been observed that nelonemdaz (0-350 μM) efficiently scavenges nitric oxide (IC50=155.8±4.88 μM), hydroxyl radicals (IC50=58.45±1.74 μM), and superoxide radicals (IC50=63.07±1.44 μM) [3]. Nelonemdaz (0.78-12.5 μM) has an IC50 of 2.21±0.11 μM and decreases ROS/RNS production generated by antimycin A in a dose-dependent manner[3]. Malondialdehyde (MDA) production is inhibited by nelonemdaz (0.19-12.5 μM) with an IC50 of 2.72±0.26 μM[3]. Nelonemdaz (0-125 μM) efficiently lowers the lipid peroxidation caused by iron ascorbate (IC50=24.56±0.07 μM)[3].
In vitro, Nelonemdaz acts as an NR2B-selective NMDA receptor antagonist and a potent ROS scavenger. It shows excellent neuroprotection against NMDA- and free radical-induced cell death. The compound is a dual-action neuroprotective agent. Detailed in vitro data are available in the primary literature. Nelonemdaz is a valuable tool for neuroprotection research. |
| ln Vivo |
Nelonemdaz (0.5–20 mg/kg; intravenously) decreases cerebral infarction in a dose-dependent manner within 24 hours following 60 minutes of middle cerebral artery occlusion (MCAO) occlusion [1]. Nelonemdaz (5 mg/kg; intravenously) guards against ischemic brain injury to gray tissue and white matter, including axons and myelin [1].
In vivo, Nelonemdaz has been evaluated as an investigational neuroprotectant. It shows neuroprotection against NMDA- and free radical-induced cell death. The compound is a dual-action NR2B-selective NMDA receptor antagonist and free radical scavenger. Further in vivo studies are needed to fully characterize its efficacy and safety profile. The compound is an investigational agent. |
| Enzyme Assay |
In vitro NMDA receptor antagonism assays for Nelonemdaz typically use primary neuronal cultures or cells expressing NR2B-containing NMDA receptors. Cells are cultured in appropriate medium and treated with Nelonemdaz at various concentrations (0.1-100 μM) prior to NMDA exposure. Cell death is assessed by LDH release or MTT assay. Calcium influx is measured using calcium-sensitive dyes. Free radical scavenging activity is assessed by DPPH, ABTS, or ROS assays. IC₅₀ values are calculated from dose-response curves. Controls include vehicle and known NMDA antagonists.
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| Cell Assay |
For cell-based assays, primary neuronal cultures or neuronal cell lines are cultured in appropriate medium. Cells are seeded in multi-well plates and pre-treated with Nelonemdaz at various concentrations (0.1-100 μM) for 30-60 minutes. Cells are exposed to NMDA or oxidative stress inducers. Cell death is assessed by LDH release, MTT assay, or propidium iodide staining. ROS levels are measured by fluorescent probes. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (260 to 300 g) (clamp occlusion model) [1]
Doses: 0.5-20 mg/kg Route of Administration: intravenous (iv) (iv)injection 5 minutes after reperfusion Experimental Results: Produced substantial neuroprotection Effect, maximizing reduction in infarct volume by 66% at doses of 2.5 to 5 mg/kg. After a dose of 5 mg/kg, no neuronal damage was observed in the most vulnerable cortical areas. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (260 to 300 g) (endoluminal wire occlusion model) [1] Doses: 5 mg/kg Route of Administration: intravenous (iv) (iv)injection 30 minutes after reperfusion Experimental Results: No changes in physiological variables, e.g. arterial pH, PCO2, PO2 and hematocrit. Cortical and striatal infarct volumes were Dramatically diminished. Dramatically diminished white matter damage in the striatum and external capsule. In vivo, Nelonemdaz may be administered to rodents via intraperitoneal (IP) or intravenous (IV) injection. The compound is formulated in a suitable vehicle such as DMSO, PEG, or saline-based solutions. For neuroprotection models (e.g., stroke, traumatic brain injury, neurodegenerative disease models), animals are dosed at various regimens. Endpoints include infarct volume, neurological deficit scoring, and histology. Blood and tissue samples are collected for pharmacokinetic and pharmacodynamic analysis. All procedures follow institutional animal care guidelines. |
| ADME/Pharmacokinetics |
Nelonemdaz (MW 383.22, C₁₅H₈F₇NO₃) is an NR2B-selective NMDA receptor antagonist and free radical scavenger. It is soluble in DMSO (≥112.5 mg/mL). The compound is an investigational neuroprotectant. Detailed pharmacokinetic parameters are available from preclinical studies. The compound is typically stored at -20°C. It is for research purposes.
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| Toxicity/Toxicokinetics |
Toxicology data for Nelonemdaz are available from preclinical studies. As an NMDA receptor antagonist, potential effects on normal glutamatergic signaling should be considered. The compound is an investigational agent and is for research use only. Standard safety pharmacology and toxicology studies have been conducted. The compound should be handled with standard laboratory safety precautions.
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| References |
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| Additional Infomation |
Nelonemdaz (Neu2000, Salfaprodil free base) is a research-grade investigational neuroprotectant. Its primary applications include neuroscience, neuroprotection research, and drug discovery. The compound is not approved for clinical use and has not completed clinical trials. It is commercially available from various chemical suppliers for research purposes only. Its mechanism involves dual-action NR2B-selective NMDA receptor antagonism and free radical scavenging.
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| Molecular Formula |
C15H8F7NO3
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|---|---|
| Molecular Weight |
383.22
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| Exact Mass |
383.039
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| CAS # |
640290-67-1
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| Related CAS # |
Nelonemdaz potassium;916214-57-8
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| PubChem CID |
9951955
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.35
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HABROHXUHNHQMY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8F7NO3/c16-10-7(11(17)13(19)9(12(10)18)15(20,21)22)4-23-5-1-2-8(24)6(3-5)14(25)26/h1-3,23-24H,4H2,(H,25,26)
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| Chemical Name |
2-hydroxy-5-[[2,3,5,6-tetrafluoro-4-(trifluoromethyl)phenyl]methylamino]benzoic acid
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| Synonyms |
Neu2000; Neu-2000-KL; Neu-2000
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 112.5 mg/mL (~293.57 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6095 mL | 13.0473 mL | 26.0947 mL | |
| 5 mM | 0.5219 mL | 2.6095 mL | 5.2189 mL | |
| 10 mM | 0.2609 mL | 1.3047 mL | 2.6095 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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