Tofisopam
Based on 1 Customer Validation
Tofisopam, a 2,3-benzodiazepine compound, is an orally active anxiolytic agent. Tofisopam can inhibit phosphodiesterase PDE isoenzyme activity, withIC50 values of 2.11 μM, 1.98 μM, 0.42 μM, and 0.92 μM for PDE-2A3, PDE-3A, PDE-4A1, and PDE-10A1, respectively. Tofisopam can be used for the study of anxiety.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.94%
- CAS 番号: 22345-47-7
- 分子式: C22H26N2O4
- 分子量:382.45
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
PDE2A3 2.11 μM (IC50) |
PDE3A 1.98 μM (IC50) |
PDE4A1 0.42 μM (IC50) |
PDE10A1 0.92 μM (IC50) |
体内実験
Tofisopam is an anxiolytic without sedative-hypnotic, muscle relaxant or anticonvulsive effects[1].
Tofisopam administration at a dose of 50 mg/kg for seven days improves the impaired cognitive performance, enhances the attenuated synaptic transmission in the hippocampus, increases proliferation in subgranular zones, and improves the decrease in astrocytes in amnesic rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Albino Swiss mice (25-30 g)[1]
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Dosage:50 mg/kg
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Administration:i.p.; twice daily on 5 days per week; for19 days
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Result:In parallel to repeated doses of Dizocilpine 0.2 mg/kg i.p. can ameliorate dizocilpine-induced prolongation of immobility.
化学情報
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CAS 番号 22345-47-7
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性状 Solid
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分子量 382.45
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分子式 C22H26N2O4
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Color White to off-white
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SMILES
CC1=NN=C(C2=CC=C(OC)C(OC)=C2)C3=CC(OC)=C(OC)C=C3C1CC
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別名
Tofisopam
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (32.68 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 1.25 mg/mL (3.27 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.27 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
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.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Rundfeldt C, et al. The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis[J]. Journal of neural transmission, 2010, 117: 1319-1325. [Content Brief]
[2]. Umut İrfan Üçel, et al. Antiamnesic effects of tofisopam against scopolamine-induced cognitive impairments in rats. Pharmacol Biochem Behav. 2020 Mar;190:172858. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL | 65.3680 mL |
| 5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL | 13.0736 mL | |
| 10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL | 6.5368 mL | |
| 15 mM | 0.1743 mL | 0.8716 mL | 1.7431 mL | 4.3579 mL | |
| 20 mM | 0.1307 mL | 0.6537 mL | 1.3074 mL | 3.2684 mL | |
| 25 mM | 0.1046 mL | 0.5229 mL | 1.0459 mL | 2.6147 mL | |
| 30 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1789 mL |
Tofisopam 関連分類
HY-A0165 関連分類
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