| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
NMDA[1]
NR2B subunit of the NMDA receptor (uncompetitive antagonist). Also acts as a free radical scavenger. |
|---|---|
| ln Vitro |
At dosages as low as 30 μM, nelonemdaz potassium (10-300 μM) exhibits apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA)[1]. In a concentration-dependent manner, nelonemdaz potassium (10-500 μM) suppresses the electrophysiologic response of cultured cortical neurons to 300 μM NMDA[1]. Even at dosages of 0.1 to 0.3 μM, nelonemdaz potassium (0.1-1 μM) significantly reduces Fe2+-induced neurotoxicity[1]. Superoxide radicals (IC50=63.07±1.44 μM), nitric oxide (IC50=155.8±4.88 μM), and hydroxyl radicals (IC50=58.45±1.74 μM) are all efficiently scavenged by nelonemdaz potassium (0-350 μM)[3]. With an IC50 of 2.21±0.11 μM, nelonemdaz potassium (0.78-12.5 μM) reduces the amount of ROS/RNS production generated by antimycin A in a dose-dependent manner [3]. With an IC50 of 2.72±0.26 μM, nelonemdaz potassium (0.19-12.5 μM) suppresses the production of malondialdehyde (MDA)[3]. Nelonemdaz potassium (0-125 μM) efficiently lowers the lipid peroxidation caused by iron ascorbate (IC50= 24.56±0.07 μM)[3].
Nelonemdaz potassium is an NR2B-selective and uncompetitive antagonist of the NMDA receptor. It exhibits remarkable neuroprotection against cell death induced by both NMDA and free radicals. Unlike most pure NR2B antagonists, it functions as both a moderate NMDA receptor antagonist and a potent, cell-permeable free radical scavenger with nanomolar-range antioxidant efficacy. |
| ln Vivo |
Nelonemdaz potassium (0.5–20 mg/kg; IV) significantly and dose-dependently decreases cerebral infarct developing 24 hours after 60 minutes of middle cerebral artery occlusion (MCAO) occlusion[1]. Nelonemdaz potassium (5 mg/kg; IV) guards against ischemic brain injury in both gray and white matter, including axons and myelin[1].
In vivo, Nelonemdaz potassium is being investigated for its neuroprotective effects in models of excitotoxicity and oxidative stress. Its dual mechanism of action—NMDA receptor antagonism and free radical scavenging—provides broad neuroprotection. It has been studied for its potential in treating stroke, traumatic brain injury, and neurodegenerative diseases. |
| Enzyme Assay |
In vitro receptor binding assays for Nelonemdaz potassium are performed to evaluate its affinity for the NR2B subunit of the NMDA receptor. Radioligand binding studies using membrane preparations from cells expressing NMDA receptors are conducted. The compound's ability to displace a specific radiolabeled ligand, such as [3H]-MK-801, is measured to calculate its binding affinity. Functional assays, such as measuring NMDA-induced calcium influx, are used to confirm its uncompetitive antagonist activity.
|
| Cell Assay |
In vitro cell-based assays are conducted using neurons or cell lines expressing NMDA receptors. The cells are treated with NMDA in the presence or absence of Nelonemdaz potassium, and cell viability is assessed to measure its neuroprotective effects. Its antioxidant activity is evaluated by measuring its ability to scavenge free radicals and protect cells from oxidative stress-induced cell death.
|
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (260 to 300 g) (clip occlusion model)[1]
Doses: 0.5-20 mg/ kg Route of Administration: Iv administration 5 mins after reperfusion Experimental Results: Produced a large neuroprotective effect, with a maximal reduction in infarct volume of 66% at doses of 2.5 to 5 mg/kg. Not observed neuronal damage in the most vulnerable cortical area after administration of 5 mg/kg. Animal/Disease Models: Male SD (Sprague-Dawley) rats (260 to 300 g) (intraluminal thread occlusion model)[1] Doses: 5 mg/kg Route of Administration: Iv administration 30 mins after reperfusion Experimental Results: Did not change physiological variables such as arterial pH, PCO2, PO2, and hematocrit. decreased infarct volume evolving in the cortex and the striatum substantially. decreased white matter damage in the striatum and external capsule markedly. In vivo animal studies are conducted in models of stroke, traumatic brain injury, and neurodegenerative diseases to evaluate the neuroprotective effects of Nelonemdaz potassium. The compound is administered via various routes, and its effects on infarct volume, neurological deficits, and cognitive function are assessed. Its ability to reduce oxidative stress and excitotoxicity in the brain is also evaluated. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for Nelonemdaz potassium. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments. The compound's ability to cross the blood-brain barrier is a key parameter for its use in CNS research.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for Nelonemdaz potassium. As an NMDA receptor antagonist and antioxidant, its toxicity profile would be expected to be related to its mechanism of action. NMDA receptor antagonists can cause psychotomimetic effects, while antioxidants are generally well-tolerated.
|
| References |
|
| Additional Infomation |
Nelonemdaz potassium (Salfaprodil; Neu2000 potassium) is an NR2B-selective and uncompetitive NMDA receptor antagonist and a free radical scavenger. It exhibits neuroprotection against cell death induced by both NMDA and free radicals. Unlike most pure NR2B antagonists, it functions as both a moderate NMDA receptor antagonist and a potent free radical scavenger. It is a research compound and is not approved for human therapeutic use.
|
| Molecular Formula |
C15H8F7KNO3
|
|---|---|
| Molecular Weight |
422.316049575806
|
| Exact Mass |
420.995
|
| CAS # |
916214-57-8
|
| Related CAS # |
Nelonemdaz;640290-67-1
|
| PubChem CID |
23684338
|
| Appearance |
Off-white to light yellow solid powder
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
27
|
| Complexity |
496
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[K].O=C(C1C(O)=CC=C(NCC2C(F)=C(F)C(C(F)(F)F)=C(F)C=2F)C=1)O
|
| InChi Key |
KLOANMLPWLPVSW-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C15H8F7NO3.K/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);/q;+1/p-1
|
| Chemical Name |
potassium;2-hydroxy-5-[[2,3,5,6-tetrafluoro-4-(trifluoromethyl)phenyl]methylamino]benzoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 200 mg/mL (474.71 mM)
|
|---|---|
| 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 | 2.3679 mL | 11.8394 mL | 23.6787 mL | |
| 5 mM | 0.4736 mL | 2.3679 mL | 4.7357 mL | |
| 10 mM | 0.2368 mL | 1.1839 mL | 2.3679 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
