Padsevonil
Based on 2 publication(s) in Google Scholar
Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
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- 純度: 99.65%
- CAS 番号: 1294000-61-5
- 分子式: C14H14ClF5N4O2S
- 分子量:432.80
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
MedChemExpress（MCE）の使用を引用している文献 Padsevonil
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生物活性
Padsevonil (0.01-30 µM) regulates GABAAR activity through allosteric sites on the receptor in CHO cells that stably express human α1β2γ2 GABAAR with an EC50 of 138 nM[1].
Padsevonil (0-30 µM) enhances natural GABAAR activity in a concentration-dependent manner in primary rat neurons with an EC50 of 208 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Padsevonil (0.14-30 mg/kg; intraperitoneal injection; single dose) has a protective effect in a rodent model of chronic epilepsy [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kainate treated male C57BL/6 mice[2]
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Dosage:1, 3, 10 and 30 mg/kg
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Administration:Intraperitoneal injection (i.p.); single dose
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Result:Significantly decreased the number of hippocampal paroxysmal discharges in dose-dependent manner.
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Animal Model:Platinum electrodes treated male Wistar rats[2]
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Dosage:0.14, 0.43, 1.38 and 4.33 mg/kg
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Administration:Intraperitoneal injection (i.p.); single dose
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Result:Produced dose-related suppression in the cumulative duration of spontaneous spike and wave discharges, and the suppression was almost complete at a dose of 4.33 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1294000-61-5
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性状 Solid
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分子量 432.80
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分子式 C14H14ClF5N4O2S
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Color White to off-white
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SMILES
O=C1N(C[C@@H](CC(F)(F)Cl)C1)CC(N(N=C(COC)S2)C2=N3)=C3C(F)(F)F
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別名
UCB-0942
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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 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Structural pharmacology of SV2A reveals an allosteric modulation mechanism in the major facilitator superfamily. [Abstract]2025 Nov 28;16(1):10748. PMID: 41315229 -
Pharmacol Rep
2024 Oct;76(5):1055-1066. PMID: 39028384
溶剤 & 溶解度
DMSO : 100 mg/mL (231.05 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (5.78 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.
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 (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Niespodziany I, et al. Functional characterization of the antiepileptic drug candidate, padsevonil, on GABAA receptors. Epilepsia. 2020 May;61(5):914-923. [Content Brief]
[2]. Leclercq K, et al. Pharmacological Profile of the Novel Antiepileptic Drug Candidate Padsevonil: Characterization in Rodent Seizure and Epilepsy Models. J Pharmacol Exp Ther. 2020 Jan;372(1):11-20. [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 |
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| DMSO | 1 mM | 2.3105 mL | 11.5527 mL | 23.1054 mL | 57.7634 mL |
| 5 mM | 0.4621 mL | 2.3105 mL | 4.6211 mL | 11.5527 mL | |
| 10 mM | 0.2311 mL | 1.1553 mL | 2.3105 mL | 5.7763 mL | |
| 15 mM | 0.1540 mL | 0.7702 mL | 1.5404 mL | 3.8509 mL | |
| 20 mM | 0.1155 mL | 0.5776 mL | 1.1553 mL | 2.8882 mL | |
| 25 mM | 0.0924 mL | 0.4621 mL | 0.9242 mL | 2.3105 mL | |
| 30 mM | 0.0770 mL | 0.3851 mL | 0.7702 mL | 1.9254 mL | |
| 40 mM | 0.0578 mL | 0.2888 mL | 0.5776 mL | 1.4441 mL | |
| 50 mM | 0.0462 mL | 0.2311 mL | 0.4621 mL | 1.1553 mL | |
| 60 mM | 0.0385 mL | 0.1925 mL | 0.3851 mL | 0.9627 mL | |
| 80 mM | 0.0289 mL | 0.1444 mL | 0.2888 mL | 0.7220 mL | |
| 100 mM | 0.0231 mL | 0.1155 mL | 0.2311 mL | 0.5776 mL |
Padsevonil 関連分類
HY-109009 関連分類
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