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Moclobemide (Ro 111163) Reversible inhibitor of MAO-A

Catalog No.A4370
Size Price Stock Qty
10mM (in 1mL DMSO)
$50.00
In stock
10mg
$50.00
In stock
50mg
$190.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Moclobemide (Ro 111163)

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Chemical Properties

Cas No. 71320-77-9 SDF Download SDF
Synonyms N/A
Chemical Name 4-chloro-N-(2-morpholin-4-ylethyl)benzamide
Canonical SMILES C1COCCN1CCNC(=O)C2=CC=C(C=C2)Cl
Formula C13H17ClN2O2 M.Wt 268.74
Solubility ≥9.85 mg/mL in DMSO, ≥48.3 mg/mL in EtOH with ultrasonic, <2.3 mg/mL in H2O Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Moclobemide is a reversible inhibitor of monoamine oxidase-A (MAO-A) with IC50 value of 10μM [1].

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. The IC50 values of MAO-A and MAO-B in the assay are 6mM and 1000mM, respectively. In ex vivo animal experiments, moclobemide produces an inhibition of 80% in the brain and liver. Additionally, the long-term administration of high doses of moclobemide is found to down-regulate β-adrenoceptors and increase the agonist binding affinity of α1-adrenoceptors. Moreover, moclobemide is rapidly and almost completely absorbed after oral administration. The bioavailability of moclobemide is about 50% after a single administration of 100 mg [2].

References:
[1] Pisani L, Barletta M, Soto-Otero R, Nicolotti O, Mendez-Alvarez E, Catto M, Introcaso A, Stefanachi A, Cellamare S, Altomare C, Carotti A. Discovery, biological evaluation, and structure-activity and -selectivity relationships of 6'-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-methylacetamides, a novel class of potent and selective monoamine oxidase inhibitors. J Med Chem. 2013 Mar 28;56(6):2651-64.
[2] Nair NP, Ahmed SK, Kin NM. Biochemistry and pharmacology of reversible inhibitors of MAO-A agents: focus on moclobemide. J Psychiatry Neurosci. 1993 Nov;18(5):214-25.