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Purity: ≥98%
Moclobemide (Ro-111163; Ro11-1163; Ro 11-1163; Amira; Aurorix; Clobemix; Depnil; Manerix) is a novel, potent, reversible monoamine oxidase MAO-A (5-HT) inhibitor with anti-depressant and anti-anxiety effects. It inhibits MAO-A with an IC50 of 6.1 μM and is mainly used for the treatment of depression and social anxiety. Moclobemide is a prototype of RIMA agents. It is found to possess antidepressant efficacy with less risk of fatal side-effects like hypertensive crisis. Moclobemide shows a weak but specific inhibition of MAO-A in the in vitro assay using rat brain homogenates.
| ln Vitro |
PC12 cell growth is inhibited by NMDA (600 µM for three days). Moclobemide (2 and 10 µM) stimulates PC12 cells treated with NMDA to proliferate more rapidly[2].
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| ln Vivo |
Moclobemide is a monoamine oxidase inhibitor that elevates norepinephrine and 5-HT levels in the brain. In animal behavior models, moclobemide (40 mg/kg) is effective[2].
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| Cell Assay |
Cell Cycle Analysis[2]
Cell Types: PC12 cell line Tested Concentrations: Moclobemide (2 and 10 µM); N-methylaspartate (NMDA) (600 µM) Incubation Duration: 3 days Experimental Results: Treatment with NMDA Dramatically decreased the percentage of S-phase, while the percentage of other cell cycle phases did not change Dramatically .However, the percentage of S-phase increased in the presence of Moclobemide. |
| Animal Protocol |
Animal/Disease Models: Chronically stressed male mice (18± 2 g) of the Kunming strain[2]
Doses: 40 mg/kg Route of Administration: Ip; daily Experimental Results: BDNF level in the hippocampal subfields including subgranule zone diminished in stressed mice compared with normal control. Chronic treatment with Moclobemide could reverse these changes. |
| References |
[1]. Nafiz Öncü Can, et al. Synthesis of New Hydrazone Derivatives for MAO Enzymes Inhibitory Activity. Molecules. 2017 Aug 20;22(8):1381.
[2]. Yun-feng Li, et al. Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice. Acta Pharmacol Sin. 2004 Nov;25(11):1408-12. |
| Molecular Formula |
C13H17CLN2O2
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| Molecular Weight |
268.74
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| CAS # |
71320-77-9
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| Related CAS # |
Moclobemide-d4
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| SMILES |
O=C(NCCN1CCOCC1)C2=CC=C(Cl)C=C2
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| InChi Key |
YHXISWVBGDMDLQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H17ClN2O2/c14-12-3-1-11(2-4-12)13(17)15-5-6-16-7-9-18-10-8-16/h1-4H,5-10H2,(H,15,17)
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| Chemical Name |
4-Chloro-N-[2-(4-morpholinyl)ethyl]benzamide
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| Synonyms |
Ro11-1163; Ro 11-1163; Ro 111163; Moclobemide; Ro111163; Ro-111163; trade name: Amira; Aurorix; Clobemix; Depnil; Manerix.
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.30 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 (9.30 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 (9.30 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 | 3.7211 mL | 18.6053 mL | 37.2107 mL | |
| 5 mM | 0.7442 mL | 3.7211 mL | 7.4421 mL | |
| 10 mM | 0.3721 mL | 1.8605 mL | 3.7211 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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