Eliprodil
Based on 1 Customer Validation
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.65%
- CAS 番号: 119431-25-3
- 分子式: C20H23ClFNO
- 分子量:347.85
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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
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生物活性
|
NMDA Receptor |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | IC50 |
1.4 μM
Compound: 2
|
In vitro inhibitory concentration against NMDA responses at NR1A/2B receptors expressed in Xenopus oocytes
In vitro inhibitory concentration against NMDA responses at NR1A/2B receptors expressed in Xenopus oocytes
|
[PMID: 10425109] |
| Oocyte | IC50 |
100 μM
Compound: 2
|
In vitro inhibitory concentration against NMDA responses at cloned NR1A/2A receptors expressed in Xenopus oocytes
In vitro inhibitory concentration against NMDA responses at cloned NR1A/2A receptors expressed in Xenopus oocytes
|
[PMID: 10425109] |
| Oocyte | IC50 |
100 μM
Compound: 2
|
In vitro inhibitory concentration against NMDA responses at NR1A/2C receptors expressed in Xenopus oocytes
In vitro inhibitory concentration against NMDA responses at NR1A/2C receptors expressed in Xenopus oocytes
|
[PMID: 10425109] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 119431-25-3
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性状 Solid
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分子量 347.85
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分子式 C20H23ClFNO
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Color White to off-white
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SMILES
ClC(C=C1)=CC=C1C(O)CN(CC2)CCC2CC3=CC=C(F)C=C3
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別名
SL-820715
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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
溶剤 & 溶解度
DMSO : 14.29 mg/mL (41.08 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: 1.43 mg/mL (4.11 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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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-
-
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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 (269 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bath CP, et al. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur J Pharmacol. 1996 Mar 28;299(1-3):103-12. [Content Brief]
[2]. Lengyel C, et al. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br J Pharmacol. 2004 Sep;143(1):152-8. [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 | 2.8748 mL | 14.3740 mL | 28.7480 mL | 71.8701 mL |
| 5 mM | 0.5750 mL | 2.8748 mL | 5.7496 mL | 14.3740 mL | |
| 10 mM | 0.2875 mL | 1.4374 mL | 2.8748 mL | 7.1870 mL | |
| 15 mM | 0.1917 mL | 0.9583 mL | 1.9165 mL | 4.7913 mL | |
| 20 mM | 0.1437 mL | 0.7187 mL | 1.4374 mL | 3.5935 mL | |
| 25 mM | 0.1150 mL | 0.5750 mL | 1.1499 mL | 2.8748 mL | |
| 30 mM | 0.0958 mL | 0.4791 mL | 0.9583 mL | 2.3957 mL | |
| 40 mM | 0.0719 mL | 0.3594 mL | 0.7187 mL | 1.7968 mL |