Talampanel
Based on 1 publication(s) in Google Scholar
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 161832-65-1
- Formula: C19H19N3O3
- Molecular Weight:337.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Talampanel
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Neuron | IC50 |
6 μM
Compound: 4
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Inhibition of kainate-induced neurotoxicity in primary rat hippocampal neurons after 24 hrs by LDH assay
Inhibition of kainate-induced neurotoxicity in primary rat hippocampal neurons after 24 hrs by LDH assay
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[PMID: 25792143] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female mutant SOD1 Tg mice[1]
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Dosage:5 mg/kg
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Administration:Orally administration; 5 mg/kg; once a day; 2 weeks
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Result:Had a significant effect in reducing the calcium level only at the age of 12 weeks.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 161832-65-1
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Appearance Solid
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Molecular Weight 337.37
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Formula C19H19N3O3
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Color White to yellow
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SMILES
C[C@@H]1CC2=C(C=C(OCO3)C3=C2)C(C4=CC=C(N)C=C4)=NN1C(C)=O
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Synonyms
GYKI-53773; LY-300164
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
A Drug Screening Pipeline Using 2D and 3D Patient-Derived In Vitro Models for Pre-Clinical Analysis of Therapy Response in Glioblastoma. [Abstract]2021 Apr 21;22(9):4322. PMID: 33919246
Solvent & Solubility
DMSO : 100 mg/mL (296.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (564 KB)
- English - EN (564 KB)
- Français - FR (564 KB)
- Deutsch - DE (564 KB)
- Norwegian - NO (564 KB)
- Español - ES (564 KB)
- Swedish - SV (564 KB)
- Italian - IT (564 KB)
- Portuguese - PT (564 KB)
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Handling Instructions (2659 KB)
References
[1]. Paizs M, et al. Talampanel reduces the level of motoneuronal calcium in transgenic mutant SOD1 mice only if applied presymptomatically. Amyotroph Lateral Scler. 2011 Sep;12(5):340-4. [Content Brief]
[2]. Denes L, et al. Talampanel a non-competitive AMPA-antagonist attenuates caspase-3 dependent apoptosis in mouse brain after transient focal cerebral ischemia. Brain Res Bull. 2006 Jul 31;70(3):260-2. Epub 2006 Mar 31. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | 74.1026 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | 14.8205 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL | 7.4103 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9761 mL | 4.9402 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4821 mL | 3.7051 mL | |
| 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9641 mL | |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4701 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4821 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2350 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7410 mL |