2614W94 |
| Catalog No.GC31021 |
2614W94 est un inhibiteur sélectif et réversible de la monoamine oxydase-A avec un mécanisme d'inhibition compétitif et IC50 de 5 nM et Ki de 1,6 nM avec la sérotonine comme substrat.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 205187-35-5
Sample solution is provided at 25 µL, 10mM.
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2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
2614W94 shows potent inhibitory activity against MAO-A, but shows no inhibition of MAO-B at 30 nM[1].
2614W94 (5 mg/kg, p.o.) produces selective inhibition of MAO-A in brains and livers of rats. 2614W94 (5 mg/kg, p.o.) also causes an elevation of neurotransmitter amines in brain, inparticular serotonin and norepinephrine, with a concomitant decrease in their oxidized metabolites. 2614W94 (0.5, 1, 2 mg/kg, p.o.) potentiates 5-hydroxytryptophan-induced head twitches in rats in a dose-dependent manner, with an extrapolated ED50 of 1.1 mg/kg[1].
[1]. Helen L. White, et al. Biochemical and Pharmacologic Properties of 2614W94, a Reversible, Competitive Inhibitor of MonoamineOxidase-A. DRUG DEVELOPMENT RESEARCH 45:1-9 (1998).
Kinase experiment: | MAO-A and -B forms are assayed. Rat brain mito-chondrial extract is pre-incubated with the inhibitor for 15 min at 37°C in 50 mM potassium phosphate buffer (pH 7.4). Substrates [3H]serotonin (0.2 mM, 5 Ci/mol) and [14C]β-phene-thylamine (10 µM, 3 Ci/mol) are then added, and incubation at 37°C is continued for 20 min. Blank assays contain 2 mM pargyline to inhibit all MAO activity. The reaction is terminated with 0.2 mL of 2 N HCl, and products are extracted with 6 mL of ethyl acetate/toluene (1:1). A 4 mL aliquot of the organic layer is countedin 10 mL of Ecolite in a scintillation spectrometer programmed for double-label counting. Assays are performed in triplicate unless otherwise indicated. At the above concentrations, serotonin is a selective substrate for MAO-A, and β-phenethylamine is aselective substrate for MAO-B. |
Animal experiment: | Rats: Nonfasted Sprague-Dawley male rats (250-350 g) are dosed by gavage with 0.5% methyl cellulose or with 2614W94 or other compounds suspended in the methyl cellulose vehicle. For all groups, n = 3 unless otherwise specified. For oral administration, dosing volume is 10 mL/kg of body weight. For intravenous dosing, the vehicle is a mixture of PEG 400 (polyethylene glycol; molecular weight, 400), ethanol, and physiologic saline in a volume ratio of 1.5/1.5/1.0, respectively, and the dosing volume is 1 mL/kg. After dosing, rats are returned to their cages and allowed free access to water. Any animals kept overnight are also given food. Death is by CO2 asphyxiation, after which brains and livers are promptly removed, frozen on dry ice, and stored at -70°C. |
References: [1]. Helen L. White, et al. Biochemical and Pharmacologic Properties of 2614W94, a Reversible, Competitive Inhibitor of MonoamineOxidase-A. DRUG DEVELOPMENT RESEARCH 45:1-9 (1998). | |
| Cas No. | 205187-35-5 | SDF | |
| Canonical SMILES | CC(OC(C=C1OC2=C3C=CC=C2)=CC=C1S3(=O)=O)C(F)(F)F | ||
| Formula | C15H11F3O4S | M.Wt | 344.31 |
| Solubility | DMSO : 100 mg/mL (290.44 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9044 mL | 14.5218 mL | 29.0436 mL |
| 5 mM | 0.5809 mL | 2.9044 mL | 5.8087 mL |
| 10 mM | 0.2904 mL | 1.4522 mL | 2.9044 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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