| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
IEM-1460 targets AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate) and NMDA (N-methyl-D-aspartate) glutamate receptors. It is a selective, voltage-dependent open-channel blocker of AMPA receptors, with selectivity for calcium-permeable AMPA receptors that lack the GluA2 subunit. The IC₅₀ values are 2.6 µM for GluR2-lacking receptors and 1102 µM for GluR2-containing receptors. By blocking these receptors, IEM-1460 inhibits glutamatergic neurotransmission, which is implicated in seizure generation and excitotoxicity. This mechanism underlies its anticonvulsant effects.
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| ln Vitro |
In vitro, IEM-1460 acts as a voltage-dependent open-channel blocker of AMPA receptors with high selectivity for Ca²⁺-permeable (GluR2-lacking) AMPA receptors over GluR2-containing receptors. The compound shows IC₅₀ values of 2.6 µM and 1102 µM for these receptor subtypes, respectively. IEM-1460 also blocks NMDA receptors. Electrophysiological studies using patch-clamp techniques in cultured neurons or heterologous expression systems demonstrate the compound's ability to inhibit AMPA and NMDA receptor-mediated currents in a use- and voltage-dependent manner. The compound is used as a pharmacological tool to study AMPA receptor function.
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| ln Vivo |
In vivo, IEM-1460 has anticonvulsant (antiepileptic/antiseizure) effects. The compound blocks both AMPA and NMDA glutamate receptors, which are involved in seizure generation and propagation. Animal studies in seizure models demonstrate the compound's ability to reduce seizure frequency and severity. IEM-1460 is used as a research tool to study the role of AMPA and NMDA receptors in epilepsy and other neurological disorders. Further in vivo studies would be needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
In vitro electrophysiological assays for IEM-1460 involve patch-clamp recordings from cells expressing AMPA or NMDA receptors. The standard protocol includes whole-cell voltage-clamp recordings from cultured neurons or HEK293 cells transfected with receptor subunits. Varying concentrations of IEM-1460 (0.1-1000 µM) are applied to the recording chamber, and receptor-mediated currents are elicited by application of agonists such as glutamate or AMPA. The degree of current inhibition is measured, and IC₅₀ values are calculated from dose-response curves. Use-dependent block is assessed by repeated agonist applications.
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| Cell Assay |
Cell-based assays for IEM-1460 are conducted in cultured neurons or heterologous expression systems. Cells expressing AMPA or NMDA receptors are treated with IEM-1460 at varying concentrations (0.1-1000 µM). Receptor function is assessed by calcium imaging using fluorescent indicators (e.g., Fluo-4) or by electrophysiological recordings. For calcium-permeable AMPA receptors, calcium influx is measured in response to agonist application. Cell viability is assessed to confirm lack of cytotoxicity. The compound is also used in studies of synaptic transmission and plasticity in neuronal cultures.
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| Animal Protocol |
In vivo animal experiments for IEM-1460 are conducted in rodent seizure models. Typical protocols involve administration of the compound via intraperitoneal or intravenous injection to mice or rats. Seizures are induced by chemical agents (e.g., pentylenetetrazole, kainic acid) or by electrical stimulation. The anticonvulsant effect is assessed by measuring seizure latency, severity, and duration. EEG recordings may be performed to monitor brain activity. The compound's effects on behavior and motor function are also evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for IEM-1460 are not extensively reported. As a small molecule with a molecular weight of 454.33 g/mol and LogP of 2.021, the compound is expected to have moderate lipophilicity and ability to cross the blood-brain barrier. Solubility is in water (45.43 mg/mL) and DMSO. Storage: powder at -20°C for 3 years or 4°C for 2 years. The compound is a bromide salt of an adamantane derivative. Further PK studies would be required for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Toxicity data for IEM-1460 are limited. The compound is supplied for research use only and is not intended for human administration. As a glutamate receptor blocker with anticonvulsant effects, it may have neurological effects at high doses. Standard laboratory safety precautions should be followed. No specific toxicological studies have been published. The compound should be handled with care and stored appropriately.
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| References | |
| Additional Infomation |
IEM-1460 (CAS 121034-89-7) is a research compound supplied for laboratory use only. It is not an approved drug and has no clinical trial or marketing authorization status. The compound is a voltage-dependent open-channel blocker of AMPA receptors with selectivity for GluA2-lacking (Ca²⁺-permeable) receptors. It also blocks NMDA receptors and has anticonvulsant effects. Purity is typically ≥98%. The compound appears as a white to off-white solid powder and should be stored at -20°C or 4°C.
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| Molecular Formula |
C19H38BR2N2
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|---|---|
| Molecular Weight |
454.3264
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| Exact Mass |
452.14
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| CAS # |
121034-89-7
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| Related CAS # |
IEM-1460; 121034-89-7
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| PubChem CID |
6604954
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| Appearance |
White to off-white solid powder
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| LogP |
2.021
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[N+](C)(C)CCCCCNCC12C[C@H](C3)C[C@H](C[C@H]3C2)C1.Br.[Br-]
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| InChi Key |
CQTDZUSQSTUZDA-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C19H37N2.2BrH/c1-21(2,3)8-6-4-5-7-20-15-19-12-16-9-17(13-19)11-18(10-16)14-19;;/h16-18,20H,4-15H2,1-3H3;2*1H/q+1;;/p-1
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| Chemical Name |
5-(1-adamantylmethylamino)pentyl-trimethylazanium;bromide;hydrobromide
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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 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~220.1 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.50 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 2.5 mg/mL (5.50 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 2.5 mg/mL (5.50 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2010 mL | 11.0052 mL | 22.0104 mL | |
| 5 mM | 0.4402 mL | 2.2010 mL | 4.4021 mL | |
| 10 mM | 0.2201 mL | 1.1005 mL | 2.2010 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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