| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Lauflumide targets multiple receptors and transporters. It has α1B-AR agonist activity (adrenergic receptor alpha-1b) and acts as a central nervous system stimulant. It exhibits MOP (mu-opioid receptor) agonist activity, which may help mitigate opioid withdrawal symptoms while preventing full opioid reinforcement. It also has partial OX2R (orexin receptor 2) agonist activity, aiding in circadian rhythm regulation. Lauflumide also functions as a dopamine reuptake inhibitor (DRI).
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| ln Vitro |
In vitro, lauflumide has been characterized for its receptor binding and transporter inhibition activities. Receptor binding assays reveal that lauflumide achieves potent dopaminergic activity without the systemic adrenergic liabilities associated with classical stimulants. It exhibits α1B-AR agonist activity, MOP agonist activity, and partial OX2R agonist activity. These activities suggest that lauflumide may have a unique pharmacological profile distinct from modafinil, with potential applications in cognitive enhancement and addiction research.
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| ln Vivo |
In vivo, lauflumide is a wakefulness-promoting research compound structurally related to modafinil. It may be used to enhance cognitive abilities. Its primary industrial and research value lies in its superior potency, distinct metabolic profile, and targeted dopaminergic activity. However, detailed in vivo efficacy data are limited in publicly available sources. The compound is not approved for clinical use and is available only for research purposes.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for lauflumide typically involve screening against a panel of receptors and transporters to characterize its pharmacological profile. Radioligand binding assays are used to measure affinity for α1B-AR, MOP, OX2R, and dopamine transporter (DAT). Functional assays (e.g., cAMP accumulation, calcium flux, or GTPγS binding) are used to assess agonist or antagonist activity at these targets. Dopamine reuptake inhibition is assessed using synaptosomal uptake assays with radiolabeled dopamine.
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| Cell Assay |
In vitro cell-based assays for lauflumide involve culturing cells expressing the relevant receptors or transporters and treating them with the compound to assess functional activity. For α1B-AR activity, calcium flux or IP3 accumulation is measured. For MOP activity, cAMP accumulation or GTPγS binding is assessed. For OX2R activity, calcium flux or other downstream signaling is measured. For dopamine transporter inhibition, cells expressing DAT are used to measure uptake of radiolabeled dopamine. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for lauflumide would typically involve rodent models to assess wakefulness-promoting, cognitive-enhancing, or addiction-related effects. Standard protocols for wakefulness-promoting agents include the rat or mouse sleep/wake EEG/EMG model, where the compound is administered and sleep/wake parameters are monitored. For cognitive enhancement, models such as the Morris water maze or novel object recognition test may be used. For addiction research, models of opioid withdrawal or self-administration may be employed. No standardized protocol is available.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of lauflumide have not been extensively characterized. As a structural analog of modafinil, it is expected to have good oral bioavailability and a favorable metabolic profile. Modafinil is well absorbed orally, reaches peak plasma concentrations in 2-4 hours, and has a half-life of approximately 12-15 hours. Lauflumide is expected to have a distinct metabolic profile compared to modafinil. No specific PK data are available.
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| Toxicity/Toxicokinetics |
The toxicity profile of lauflumide has not been systematically evaluated. As a research compound, it is not intended for human use. Modafinil and its analogs are generally well-tolerated, but can cause headache, nausea, nervousness, and insomnia. At high doses, they may cause cardiovascular effects or psychiatric symptoms. Standard toxicology assessments for lauflumide would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References | |
| Additional Infomation |
Lauflumide (bisfluoromodafinil, flmodafinil) is a synthetic small-molecule research compound structurally related to modafinil. It exhibits α1B-AR agonist, MOP agonist, and partial OX2R agonist activities, and functions as a dopamine reuptake inhibitor. The compound has potential for cognitive enhancement and wakefulness promotion. Lauflumide is a research compound not approved for clinical use. It is available only for in vitro and in vivo pharmacological studies.
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| Molecular Formula |
C15H13F2NO2S
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|---|---|
| Molecular Weight |
309.33
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| Exact Mass |
309.063
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| CAS # |
90280-13-0
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| PubChem CID |
13271852
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
558.7±50.0 °C at 760 mmHg
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| Melting Point |
78-80 °C
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| Flash Point |
291.7±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
1.27
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
21
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| Complexity |
356
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YEAQNUMCWMRYMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13F2NO2S/c16-12-5-1-10(2-6-12)15(21(20)9-14(18)19)11-3-7-13(17)8-4-11/h1-8,15H,9H2,(H2,18,19)
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| Chemical Name |
2-[bis(4-fluorophenyl)methylsulfinyl]acetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (323.28 mM）
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2328 mL | 16.1640 mL | 32.3279 mL | |
| 5 mM | 0.6466 mL | 3.2328 mL | 6.4656 mL | |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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