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[1] bioRxiv preprint
Purity: ≥98%
ln Vitro |
In human brain synaptosomes and human liver mitochondria, bifemelane inhibits MAO-A in a dose-dependent manner with Kis values of 4.2±0.2 and 14.1±0.7 μM, respectively [1]. In human brain synaptosomes and human liver mitochondria, bifemelane inhibits MAO-B activity in a dose-dependent manner with Kis values of 46.0±3.6 and 65.2±7.0 μM, respectively [1].
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ln Vivo |
Bifemelane (20-80 mg/kg; intraperitoneal injection) decreases exploratory activity in the open field test in a dose-dependent manner [3]. In the forced swim test, Bifemelane (20-80 mg/kg; intraperitoneal injection) shortens the immobility period [3], however the dose dependence is not evident and the maximum dosage of 20 mg/kg has been attained.
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Animal Protocol |
Animal/Disease Models: Wistar male rats (230-270 g) Reserpine-induced hypothermia [3]
Doses: 20, 40, 80 mg/kg Route of Administration: Single intraperitoneal (ip) injection Experimental Results: Reserpine-induced hypothermia If it is too low, the maximum temperature will be diminished by 10℃. |
References |
[1]. Naoi M, et, al. 4-(O-benzylphenoxy)-N-methylbutylamine (bifemelane) and other 4-(O-benzylphenoxy)-N-methylalkylamines as new inhibitors of type A and B monoamine oxidase. J Neurochem. 1988 Jan; 50(1): 243-7.
[2]. Fasipe OJ, et, al. The emergence of new antidepressants for clinical use: Agomelatine paradox versus other novel agents. IBRO Rep. 2019 Jan 9; 6:95-110. [3]. Moryl E, et, al. Potential antidepressive properties of amantadine, memantine and bifemelane. Pharmacol Toxicol. 1993 Jun; 72(6): 394-7. |
Molecular Formula |
C18H24CLNO
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Molecular Weight |
305.846
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Exact Mass |
269.178
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CAS # |
62232-46-6
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Related CAS # |
Bifemelane;90293-01-9
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SMILES |
CNCCCCOC1=CC=CC=C1CC2=CC=CC=C2.Cl
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Synonyms |
MCI-2016 MCI 2016 MCI2016Bifemelane Bifemelanum Bifemelane HCl
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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 : ~250 mg/mL (~817.42 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.80 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 20.8 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: ≥ 2.08 mg/mL (6.80 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 20.8 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: ≥ 2.08 mg/mL (6.80 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 | 3.2696 mL | 16.3479 mL | 32.6958 mL | |
5 mM | 0.6539 mL | 3.2696 mL | 6.5392 mL | |
10 mM | 0.3270 mL | 1.6348 mL | 3.2696 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.