Lorediplon
Based on 1 Customer Validation
Lorediplon is a binder predicted via molecular docking to bind SYT1 and SYN2, with affinity for both targets, and it forms stable complexes to regulate protein function. Lorediplon is also a non-benzodiazepine compound that modulates the GABA receptor and exhibits differential activity toward the α1 subunit. Lorediplon can be used in Alzheimer's disease research.
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- Pureza : 99.88%
- No. CAS: 917393-39-6
- Fòrmula: C20H15FN4O2S
- Peso molecular:394.42
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Almacenamiento: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
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
Lorediplon binds potently to purified SYT1 protein with a binding energy of -7.7 kcal/mol, forming a complex stabilized by hydrogen bonding and hydrophobic interactions[1].
Lorediplon binds to purified SYN2 protein with a binding energy of -6.3 kcal/mol, forming a complex stabilized by multiple hydrogen bonds and hydrophobic interactions[1].
Lorediplon (last 10 ns of 100 ns simulation trajectories) forms thermodynamically stable complexes with SYT1 and SYN2, with average MM-PBSA binding free energies of -22.56 kJ/mol and -21.54 kJ/mol, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 917393-39-6
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Appearance Solid
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Peso molecular 394.42
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Fòrmula C20H15FN4O2S
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Color Light yellow to yellow
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SMILES
CC(N(C1=CC(C2=CC=NC3=C(C(C4=CC=CS4)=O)C=NN23)=CC=C1F)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (253.54 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (6.34 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.34 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 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.
Protocolo
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureza y Documentación
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Ficha de datos (290 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.5354 mL | 12.6768 mL | 25.3537 mL | 63.3842 mL |
| 5 mM | 0.5071 mL | 2.5354 mL | 5.0707 mL | 12.6768 mL | |
| 10 mM | 0.2535 mL | 1.2677 mL | 2.5354 mL | 6.3384 mL | |
| 15 mM | 0.1690 mL | 0.8451 mL | 1.6902 mL | 4.2256 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2677 mL | 3.1692 mL | |
| 25 mM | 0.1014 mL | 0.5071 mL | 1.0141 mL | 2.5354 mL | |
| 30 mM | 0.0845 mL | 0.4226 mL | 0.8451 mL | 2.1128 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5846 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5071 mL | 1.2677 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0564 mL | |
| 80 mM | 0.0317 mL | 0.1585 mL | 0.3169 mL | 0.7923 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6338 mL |
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