| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
The primary targets of Adrafinil are the central nervous system pathways, but its mechanism is not fully understood. It is believed to work by increasing the levels of certain neurotransmitters, including dopamine and glutamate, in the brain. Its active metabolite modafinil is a weak dopamine transporter inhibitor, and it also modulates orexin and histamine systems. Adrafinil's actions are thought to promote wakefulness and enhance cognitive function.
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| ln Vitro |
In vitro, Adrafinil itself has limited activity, as it is a prodrug. Its metabolite modafinil has been shown to inhibit dopamine reuptake and increase extracellular dopamine levels in brain slices. In vitro studies using liver microsomes demonstrate its conversion to modafinil. The compound's ability to cross the blood-brain barrier is attributed to its active metabolite.
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| ln Vivo |
In vivo, Adrafinil has been shown to increase wakefulness and reduce excessive daytime sleepiness in animal models and humans. It improves performance in tasks requiring attention and reaction time. In rats, it increases locomotor activity and reverses reserpine-induced sedation. Its effects are dose-dependent and have a slow onset due to the need for hepatic conversion.
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| Enzyme Assay |
In vitro enzyme assays for Adrafinil measure its conversion to modafinil by liver microsomes. The activity of cytochrome P450 enzymes, particularly CYP3A4, is assessed by monitoring the formation of modafinil using HPLC. The compound's stability in plasma and liver homogenates can also be evaluated. These assays are for research purposes.
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| Cell Assay |
In vitro cell-based assays for Adrafinil are less common, as its active metabolite is the primary effector. However, neuronal cell cultures can be treated with modafinil to study its effects on dopamine transporter activity and downstream signaling. Cell viability and neurotoxicity can be assessed using standard cytotoxicity assays.
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| Animal Protocol |
In vivo animal studies for Adrafinil typically involve behavioral tests in rodents, such as the open field test, rotarod, and sleep-wake recordings. The compound is administered orally or intraperitoneally, and its effects on locomotor activity, alertness, and cognitive performance are measured. Pharmacokinetic studies monitor plasma and brain levels of modafinil. All procedures follow ethical guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Adrafinil include good oral absorption, with a peak plasma level of modafinil occurring a few hours after administration. It has a half-life of approximately 1 hour, while its metabolite modafinil has a longer half-life (12-15 hours). The compound is metabolized in the liver. Storage should be at room temperature in a dry place.
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| Toxicity/Toxicokinetics |
The toxicity profile of Adrafinil includes potential side effects such as headache, anxiety, and gastrointestinal disturbances. Hepatotoxicity has been reported, especially with chronic use, which led to its limited availability. It is classified as a research compound and is not approved for human use in many countries. Safety precautions should be followed.
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| Additional Infomation |
Adrafinil is a diarylmethane compound. Adrafinil is a mild central nervous system stimulant, commonly used to relieve excessive drowsiness and inattention in elderly patients. It is also used to prevent fatigue or prolonged sleep (off-label use). Adrafinil is not currently approved by the U.S. Food and Drug Administration (FDA) and is therefore unregulated in the United States. It was marketed under the brand name Olmifen in France and other parts of Europe until September 2011, when the French FDA re-evaluated the drug and withdrew its marketing authorization. Adrafinil is metabolized to modafinil. Drug Indications: For the relief of excessive drowsiness and inattention in elderly patients. Pharmacodynamics: Adrafinil is a prodrug; it is primarily metabolized in the body to modafinil, producing almost the same pharmacological effects. Unlike modafinil, the active metabolite must accumulate before the drug can exert its effects. When taken orally on an empty stomach, modafinil usually begins to take effect within 45 minutes to 1 hour.
Additional information: Adrafinil was marketed in France under the brand name Olmifon for a time but was withdrawn. It is now used mainly as a research chemical and is not intended for human consumption. It is a prodrug for modafinil. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C15H15NO3S
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|---|---|
| Molecular Weight |
289.3495
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| Exact Mass |
289.077
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| CAS # |
63547-13-7
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| PubChem CID |
3033226
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Melting Point |
159-1600C
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| Index of Refraction |
1.653
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| LogP |
0.77
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
318
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])C(N([H])O[H])=O)(C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O
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| InChi Key |
CGNMLOKEMNBUAI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15NO3S/c17-14(16-18)11-20(19)15(12-7-3-1-4-8-12)13-9-5-2-6-10-13/h1-10,15,18H,11H2,(H,16,17)
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| Chemical Name |
2-benzhydrylsulfinyl-N-hydroxyacetamide
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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 (~345.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (17.28 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 50.0 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: ≥ 5 mg/mL (17.28 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 50.0 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: ≥ 5 mg/mL (17.28 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 | 3.4560 mL | 17.2801 mL | 34.5602 mL | |
| 5 mM | 0.6912 mL | 3.4560 mL | 6.9120 mL | |
| 10 mM | 0.3456 mL | 1.7280 mL | 3.4560 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06646822 | Enrolling by invitation | Drug: Stimulant | Study of Stimulants in Egypt | Asmaa Ahmed Hamed Mohie Eldin | 2024-10-30 |
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