| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
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| Targets |
NMDA receptor (glutamate site). Perzinfotel is a potent, selective, and competitive NMDA receptor antagonist. It binds to the glutamate site of the NMDA receptor with high affinity (IC50 of 30 nM). The NMDA receptor is a ligand-gated ion channel that plays a critical role in excitatory neurotransmission, synaptic plasticity, and excitotoxicity. By blocking the glutamate site, Perzinfotel prevents excessive calcium influx and downstream excitotoxic signaling. The compound's competitive mechanism of action distinguishes it from non-competitive NMDA receptor antagonists. Perzinfotel has neuroprotective effects.
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| ln Vitro |
At an IC50 of 0.48 μM for NMDA-induced currents and 1.6 μM for glutamate-induced neurotoxicity, perzinfotel inhibits both types of neurotoxicity [1].
Perzinfotel is a potent NMDA receptor antagonist with high affinity for the glutamate site (IC50 of 30 nM). The compound demonstrates neuroprotective effects in vitro by preventing glutamate-induced excitotoxicity. Perzinfotel is a competitive NMDA receptor antagonist. The compound's potency and selectivity make it a valuable tool for studying NMDA receptor function and excitotoxicity. |
| ln Vivo |
Perzinfotel has been studied in vivo for its neuroprotective effects. The compound has been used in trials investigating the treatment of diabetes and diabetic neuropathy (painful conditions). By inhibiting NMDA receptor overactivation, Perzinfotel prevents excitotoxicity and has neuroprotective effects. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical and clinical studies. Perzinfotel is a competitive NMDA receptor antagonist.
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| Enzyme Assay |
NMDA receptor binding assays are performed using membranes prepared from rat brain or from cells expressing recombinant NMDA receptors. Radioligand binding studies use [³H]-MK-801 or [³H]-CGP-39653 as labeled ligands. Membrane preparations are incubated with varying concentrations of Perzinfotel and a fixed concentration of radioligand in binding buffer for 60-120 minutes. Non-specific binding is determined using excess unlabeled ligand (e.g., glutamate or NMDA). Bound radioactivity is measured by scintillation counting after filtration through GF/B filters. IC50 and Ki values are calculated by non-linear regression. The IC50 for Perzinfotel is 30 nM.
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| Cell Assay |
Cellular NMDA receptor antagonism is evaluated in primary neuronal cultures or cell lines expressing NMDA receptors. Cells are cultured in appropriate media and treated with Perzinfotel at various concentrations. NMDA-induced calcium influx is measured using fluorescent calcium indicators (Fura-2, Fluo-4). Cell viability is assessed using MTT or LDH assays to evaluate neuroprotection against excitotoxicity. Each experiment includes known NMDA receptor antagonists (e.g., AP5, MK-801) as positive controls and vehicle controls.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of excitotoxicity, stroke, diabetic neuropathy, and other neurological disorders. Perzinfotel is administered intraperitoneally or intravenously at doses determined by preclinical studies. Neuroprotective effects are assessed by measuring infarct volume, neuronal survival, and behavioral outcomes. For diabetic neuropathy studies, pain responses are assessed. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 260.18. Formula: C9H13N2O5P. CAS No.: 144912-63-0. IUPAC Name: 2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethylphosphonic acid. Synonyms: EAA-090. Purity: >98%. Appearance: Solid. Solubility: DMSO. Density: 1.60 g/cm³ (Predicted). Storage: Typically at -20°C. Perzinfotel is a potent, selective, and competitive NMDA receptor antagonist with an IC50 of 30 nM.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Perzinfotel. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As an NMDA receptor antagonist, potential adverse effects may include sedation, cognitive impairment, and psychosis-like effects. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). Perzinfotel is for research use only and not for human therapeutic use.
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| References |
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| Additional Infomation |
Perzinfotel is a dialkyl aromatic amine and tertiary amine compound. Perzinfotel has been used in trials investigating the treatment of diabetes and diabetic neuropathy (painful conditions).
Perzinfotel is also known as EAA-090. Its IUPAC name is 2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethylphosphonic acid. Perzinfotel is a potent, selective, and competitive NMDA receptor antagonist with an IC50 of 30 nM. Perzinfotel has neuroprotective effects. Perzinfotel has been used in trials investigating the treatment of diabetes and diabetic neuropathy. No regulatory approvals have been reported. Perzinfotel is for research use only. |
| Molecular Formula |
C9H13N2O5P
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|---|---|
| Molecular Weight |
260.1858
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| Exact Mass |
260.056
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| CAS # |
144912-63-0
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| PubChem CID |
6918236
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
-1.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
452
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BDABGOLMYNHHTR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H13N2O5P/c12-8-6-7(9(8)13)11(3-1-2-10-6)4-5-17(14,15)16/h10H,1-5H2,(H2,14,15,16)
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| Chemical Name |
2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)ethylphosphonic acid
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| Synonyms |
WAY-126090; EAA-090; Perzinfotel
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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 : ~20.83 mg/mL (~80.06 mM)
H2O : ~5.88 mg/mL (~22.60 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (19.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8433 mL | 19.2167 mL | 38.4335 mL | |
| 5 mM | 0.7687 mL | 3.8433 mL | 7.6867 mL | |
| 10 mM | 0.3843 mL | 1.9217 mL | 3.8433 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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