Lauflumide
Based on 1 Customer Validation
Lauflumide (BisfluoroModafinil) is a selective dopamine reuptake inhibitor and wake-promoting agent. Lauflumide inhibits the dopamine transporter (DAT). Lauflumide induces sustained wakefulness without eliciting hyperlocomotion, stereotypy or abnormal behaviors in Mus musculus (house mice). Lauflumide reduces non-rapid eye movement (NREM) sleep rebound in rats, modulates electroencephalogram (EEG) spectral composition, and produces anti-aggressive effects. Lauflumide alleviates circadian rhythm disturbances in rats, increases spontaneous activity in fatigued rats, and facilitates their recovery from severe fatigue. Lauflumide can be used in research related to excessive daytime sleepiness as well as chronic severe fatigue/chronic fatigue syndrome (CFS).
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- Pureté: 99.18%
- CAS No.: 90280-13-0
- Formule: C15H13F2NO2S
- Masse moléculaire:309.33
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Lauflumide (16-64 mg/kg; administered daily for 3 times) dose-dependently and persistently enhances spontaneous locomotor activity in fatigued rats, and the improvement of fatigue-induced circadian rhythm impairment at the 16 mg/kg dose is comparable to that of 64 mg/kg Modafinil[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 10-11 weeks old, 22-26 g)[1]
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Dosage:32 mg/kg; 64 mg/kg; 128 mg/kg; 256 mg/kg
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Administration:i.p.; single dose at light onset
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Result:Induced 160 minutes of locomotor activity at 32 mg/kg.
Induced 250 minutes of locomotor activity at 64 mg/kg.
Induced 190 minutes of locomotor activity at 128 mg/kg.
Induced 170 minutes of locomotor activity at 256 mg/kg.
Increased sleep latency to 208 minutes at 64 mg/kg (vs. 55.92 minutes for vehicle).
Extended net wakefulness duration by 151 minutes at 64 mg/kg, significantly longer than modafinil's net wakefulness duration.
Reduced light period NREM sleep to 254.41 minutes (vs. 342.02 minutes for vehicle) at 64 mg/kg.
Reduced light period REM sleep to 40.67 minutes (vs. 49.84 minutes for vehicle) at 64 mg/kg.
Reduced light period wakefulness to 223.30 minutes (vs. 273.37 minutes for vehicle) at 64 mg/kg.
Caused NREM sleep loss of -87.61 minutes and REM sleep loss of -9.18 minutes during light period at 64 mg/kg.
Increased relative power density in 0.75-3.25 Hz range and decreased relative power density in 6.25-7.25 Hz range during NREM sleep.
Decreased relative theta power density during REM sleep.
Increased relative low delta power in 0.75-1.25 Hz range during wakefulness.
Increased delta power during the first 2 time intervals post-sleep onset of recovery NREM sleep.
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Animal Model:Sprague-Dawley (male, 7-8 weeks old, chronic severe fatigue model via 7-day consecutive fatigue procedure)[2]
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Dosage:16 mg/kg; 32 mg/kg; 64 mg/kg
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Administration:three daily doses
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Result:Increased dark-phase locomotor activity significantly at 16, 32, and 64 mg/kg.
Increased light-phase locomotor activity to a lesser extent.
Reduced fatigue-induced circadian rhythm impairment at 16 mg/kg to a similar magnitude as modafinil at 64 mg/kg.
Exhibited more sustainable effect on dark-phase activity than modafinil.
Chemical Information
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CAS No. 90280-13-0
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Appearance Solid
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Masse moléculaire 309.33
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Formule C15H13F2NO2S
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Color White to off-white
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SMILES
O=C(N)CS(C(C1=CC=C(F)C=C1)C2=CC=C(F)C=C2)=O
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Synonyms
BisfluoroModafinil; CRL-40940; NLS-4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (323.28 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (8.08 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 (8.08 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.
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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (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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Instruction de manipulation (2659 KB)
Références
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 | 3.2328 mL | 16.1640 mL | 32.3279 mL | 80.8198 mL |
| 5 mM | 0.6466 mL | 3.2328 mL | 6.4656 mL | 16.1640 mL | |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL | 8.0820 mL | |
| 15 mM | 0.2155 mL | 1.0776 mL | 2.1552 mL | 5.3880 mL | |
| 20 mM | 0.1616 mL | 0.8082 mL | 1.6164 mL | 4.0410 mL | |
| 25 mM | 0.1293 mL | 0.6466 mL | 1.2931 mL | 3.2328 mL | |
| 30 mM | 0.1078 mL | 0.5388 mL | 1.0776 mL | 2.6940 mL | |
| 40 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0205 mL | |
| 50 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.6164 mL | |
| 60 mM | 0.0539 mL | 0.2694 mL | 0.5388 mL | 1.3470 mL | |
| 80 mM | 0.0404 mL | 0.2020 mL | 0.4041 mL | 1.0102 mL | |
| 100 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL |