Fmoc-DL-Leu-OH
Based on 1 Customer Validation
Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor (NTS1R) with an EC50 of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia.
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 : 99.69%
- CAS 番号: 126727-03-5
- 分子式: C21H23NO4
- 分子量:353.42
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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
- プロトコル
- 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
[2]|
NTR1 215.50 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
215.5 μM
Compound: 1
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Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay
Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay
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[PMID: 18849166] |
| CHO-K1 | EC50 |
216 nM
Compound: 6
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Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay
Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay
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[PMID: 19195889] |
| CHO-K1 | IC50 |
3.79 nM
Compound: 1
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Antagonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium elevation pretreated 30 mins before with SR-48692 by FLIPR assay
Antagonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium elevation pretreated 30 mins before with SR-48692 by FLIPR assay
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[PMID: 18849166] |
体外実験
Fmoc-DL-Leu-OH (Compound 1) acts as a partial agonist of human NTS1R expressed in CHOK1 cells, with an EC50 of 215.50 μM and a potency reaching 60% of the maximum potency of NT[1].
Fmoc-DL-Leu-OH (50 μM) exhibited agonist activity at human NTS1R expressed in CHOK1 cells, which was blocked by the selective NTS1R antagonist SR-48692 with an IC50 of 3.79 nM[1].
Fmoc-DL-Leu-OH (60 min) shows no detectable binding to human NTS1R in a [3H]neurotensin competitive binding assay performed using stably transfected CHOK1 cell membranes[1].
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 126727-03-5
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性状 Solid
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分子量 353.42
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分子式 C21H23NO4
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Color White to off-white
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SMILES
O=C(OCC1C=2C=CC=CC2C=3C=CC=CC31)NC(C(=O)O)CC(C)C
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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 : 100 mg/mL (282.95 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)
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: 2.5 mg/mL (7.07 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (7.07 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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 (275 KB)
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SDS (394 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 | 2.8295 mL | 14.1475 mL | 28.2949 mL | 70.7374 mL |
| 5 mM | 0.5659 mL | 2.8295 mL | 5.6590 mL | 14.1475 mL | |
| 10 mM | 0.2829 mL | 1.4147 mL | 2.8295 mL | 7.0737 mL | |
| 15 mM | 0.1886 mL | 0.9432 mL | 1.8863 mL | 4.7158 mL | |
| 20 mM | 0.1415 mL | 0.7074 mL | 1.4147 mL | 3.5369 mL | |
| 25 mM | 0.1132 mL | 0.5659 mL | 1.1318 mL | 2.8295 mL | |
| 30 mM | 0.0943 mL | 0.4716 mL | 0.9432 mL | 2.3579 mL | |
| 40 mM | 0.0707 mL | 0.3537 mL | 0.7074 mL | 1.7684 mL | |
| 50 mM | 0.0566 mL | 0.2829 mL | 0.5659 mL | 1.4147 mL | |
| 60 mM | 0.0472 mL | 0.2358 mL | 0.4716 mL | 1.1790 mL | |
| 80 mM | 0.0354 mL | 0.1768 mL | 0.3537 mL | 0.8842 mL | |
| 100 mM | 0.0283 mL | 0.1415 mL | 0.2829 mL | 0.7074 mL |
Fmoc-DL-Leu-OH 関連分類
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