| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Calcium-permeable AMPA receptors (CP-AMPARs / GluA2-lacking AMPA receptors).
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|---|---|
| ln Vitro |
NASPM primarily inhibits the inward rectifying and Ca2+-permeable AMPA receptors expressed in type II neurons. It has no effect on AMPA receptors in type I neurons. At -60 mV, NASPM inhibits AMPA receptors in type II neurons with an IC50 value of 0.33 µM. The inhibiting effect of NASPM on Ca2+ permeable AMPA receptors is application- and voltage-dependent [1].
Naspm selectively antagonizes calcium-permeable AMPA receptors by blocking GluA2-lacking AMPAR subtypes. It does not affect calcium-impermeable AMPA receptors (those containing GluA2). The compound inhibits CP-AMPAR-mediated currents in a concentration-dependent manner. |
| ln Vivo |
Naspm is used as a research tool to study the role of CP-AMPARs in synaptic plasticity, learning and memory, and neurodegenerative diseases. In vivo, it can modulate glutamatergic transmission and has been studied in models of ischemia and epilepsy.
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| Enzyme Assay |
AMPA receptor binding assays are performed using membrane preparations from brain tissue or cells expressing recombinant AMPA receptor subunits. Radiolabeled ligand (e.g., [3H]-AMPA) displacement or electrophysiological recordings assess the compound's activity at CP-AMPARs.
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| Cell Assay |
Neuronal cultures or cells expressing AMPA receptors (e.g., HEK-293 cells transfected with GluA1/2 or GluA1 alone) are treated with Naspm. Whole-cell patch-clamp recordings measure the inhibition of AMPA-evoked currents. The selectivity for GluA2-lacking receptors is confirmed by comparing responses in cells with and without GluA2.
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| Animal Protocol |
Animal models of neurological disorders (e.g., ischemia, epilepsy, or neurodegenerative diseases) are used to assess the in vivo effects of Naspm. The compound is administered centrally (i.c.v.) or systemically. Behavioral, electrophysiological, and histological endpoints are measured.
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| ADME/Pharmacokinetics |
Predicted to have poor oral bioavailability due to its polar nature. The compound is typically administered parenterally or centrally for in vivo studies. Brain penetration is expected to be moderate. Half-life is likely short due to rapid clearance.
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| Toxicity/Toxicokinetics |
No specific toxicity data reported for Naspm. As a research tool, it is used at concentrations that are well-tolerated in animal studies. No significant off-target effects have been reported at selective doses.
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| References | |
| Additional Infomation |
1-Naphthylacetylspermine is a type of naphthalene compound.
Naspm is a research tool for studying CP-AMPAR biology and the therapeutic potential of CP-AMPAR antagonists in neurological disorders. It has not been approved for clinical use. The compound's mechanism involves blocking the pore of calcium-permeable AMPA receptors, preventing calcium influx and downstream signaling. |
| Molecular Formula |
C22H35N4O
|
|---|---|
| Molecular Weight |
371.54000
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| Exact Mass |
370.273
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| CAS # |
122306-11-0
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| Related CAS # |
Naspm trihydrochloride;1049731-36-3
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| PubChem CID |
129695
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.062g/cm3
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| Boiling Point |
608.9ºC at 760mmHg
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| Flash Point |
322.1ºC
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| Vapour Pressure |
9.01E-15mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
4.835
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
27
|
| Complexity |
391
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C([H])([H])C1=C([H])C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])C([H])([H])C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H]
|
| InChi Key |
ZUINPPQIQARTKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H34N4O/c23-12-6-15-24-13-3-4-14-25-16-7-17-26-22(27)18-20-10-5-9-19-8-1-2-11-21(19)20/h1-2,5,8-11,24-25H,3-4,6-7,12-18,23H2,(H,26,27)
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| Chemical Name |
N-[3-[4-(3-aminopropylamino)butylamino]propyl]-2-naphthalen-1-ylacetamide
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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 : ~10 mg/mL (~26.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.70 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.70 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 10.0 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: ≥ 1 mg/mL (2.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6915 mL | 13.4575 mL | 26.9150 mL | |
| 5 mM | 0.5383 mL | 2.6915 mL | 5.3830 mL | |
| 10 mM | 0.2692 mL | 1.3458 mL | 2.6915 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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