SERT-IN-2
Based on 1 Customer Validation
SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier.
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: 98.06%
- CAS 番号: 2055228-33-4
- 分子式: C26H24F2N6
- 分子量:458.51
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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
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生物活性
IC50: 0.58 nM (SERT)[1]
SERT-IN-2 (10 mg/kg; i.p.; single dose) can cross the blood brain barrier in SD rats[1].
SERT-IN-2 (1-10 mg/kg; i.p.; single dose) inhibited serotonin uptake and potently antagonizes the p-chloroamphetamine (PCA)-induced depletion of 5-HT in the rat hypothalamus[1].
SERT-IN-2 (1-10 mg/kg; i.v.; 3 times before the test) exerts antidepressant effect in rat, reduces the immobility times in the forced swimming test (FST) in a dose-dependent manner[1].
Pharmacokinetic Analysis[1]
| Route | Dose (mg/kg) | Cmax (ng/mL) | AUC(0-t) (ng·h/mL) | T1/2 (h) | Vss (L/kg) | Cl (L/h/kg) | F (%) | |
| Rat | IV | 1 | 193 | 1340 | 7.53 | 6.41 | 11.6 | / |
| PO | 2.5 | 180 | 2790 | 7.28 | / | / | 83.28 | |
| Dog | IV | 1 | 520 | 2820 | 4.39 | 3.4 | 5.14 | / |
| PO | 5 | 794 | 7540 | 16.4 | / | / | 53.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2055228-33-4
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性状 Solid
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分子量 458.51
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分子式 C26H24F2N6
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Color White to off-white
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SMILES
N#CC1=CC2=C(NC=C2CCCN3CCN(CC3)C4=NC=C(C5=CC=C(C=C5F)F)C=N4)C=C1
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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
DMSO : 200 mg/mL (436.20 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, 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)
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: ≥ 5 mg/mL (10.90 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1810 mL | 10.9049 mL | 21.8098 mL | 54.5244 mL |
| 5 mM | 0.4362 mL | 2.1810 mL | 4.3620 mL | 10.9049 mL | |
| 10 mM | 0.2181 mL | 1.0905 mL | 2.1810 mL | 5.4524 mL | |
| 15 mM | 0.1454 mL | 0.7270 mL | 1.4540 mL | 3.6350 mL | |
| 20 mM | 0.1090 mL | 0.5452 mL | 1.0905 mL | 2.7262 mL | |
| 25 mM | 0.0872 mL | 0.4362 mL | 0.8724 mL | 2.1810 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7270 mL | 1.8175 mL | |
| 40 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3631 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0905 mL | |
| 60 mM | 0.0363 mL | 0.1817 mL | 0.3635 mL | 0.9087 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6816 mL | |
| 100 mM | 0.0218 mL | 0.1090 mL | 0.2181 mL | 0.5452 mL |
SERT-IN-2 関連分類
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