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Meclofenoxate (Centrophenoxine) HCl

Alias:
Cat No.:V1923 Purity: ≥98%
Meclofenoxate (also known as Centrophenoxine) HCl is a potent nootropic agent and an anti-aging drug used to treat the symptoms of senile dementia and Alzheimers disease, and also inhibits the activity of cholinephosphotransferase.
Meclofenoxate (Centrophenoxine) HCl
Meclofenoxate (Centrophenoxine) HCl Chemical Structure CAS No.: 3685-84-5
Product category: nAChR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
Other Sizes
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
Meclofenoxate (also known as Centrophenoxine) HCl is a potent nootropic agent and an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase. Meclofenoxate hydrochloride, an ester of dimethylethanolamine (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown to improve memory, have a mentally stimulating effect, and improve general cognition.
Meclofenoxate (Lucidril) is a compound synthesized by combining dimethylaminoethanol with p-chlorophenoxyacetic acid. Its hydrochloride salt is a white solid soluble in water. While its full action is not fully described, it has been shown to reduce lipofuscin granule accumulation in aged guinea-pigs. Histochemical studies indicate it reduces succinic and lactic dehydrogenase activity and enhances glucose-6-phosphate dehydrogenase activity, suggesting enhancement of cellular metabolism via activation of the pentose shunt pathway. It also enhances resistance of cerebral cells to oxygen deprivation in rats, mice, and rabbits. [1]
Meclofenoxate (Centrophenoxine) HCl is a central nervous system stimulant and a cholinergic agent. It has the molecular formula C12H16ClNO3·HCl and a molecular weight of 294.17 g/mol. Meclofenoxate is a prodrug of dimethylaminoethanol (DMAE) and p-chlorophenoxyacetic acid. It is used in research for its potential nootropic effects and in the treatment of cognitive disorders. The compound is believed to enhance cholinergic function in the brain, leading to improved cognitive performance. It is also studied for its potential anti-aging effects.
Biological Activity I Assay Protocols (From Reference)
Targets
Meclofenoxate HCl targets the cholinergic system in the brain. As a prodrug of dimethylaminoethanol (DMAE), it is believed to increase the availability of choline, a precursor to the neurotransmitter acetylcholine. By enhancing cholinergic function, it may improve cognitive processes such as memory and learning. It may also have effects on cerebral circulation and metabolism. Its mechanism as a cognitive enhancer is primarily attributed to its action on the cholinergic system.
ln Vitro
In vitro, Meclofenoxate HCl has been studied for its effects on neuronal cells. It is a prodrug that is metabolized to DMAE, which can serve as a precursor for acetylcholine synthesis. Studies have shown that it can increase the release of acetylcholine in brain slices. It has also been investigated for its antioxidant properties and its ability to protect cells from oxidative stress. These in vitro studies provide a basis for its potential neuroprotective and cognitive-enhancing effects.
ln Vivo
In vivo studies in aged guinea-pigs demonstrated that Meclofenoxate markedly reduces accumulation of lipofuscin granules in neurons [1].
In rats, mice, and rabbits, Meclofenoxate enhanced resistance of cerebral cells to various forms of oxygen deprivation including cyanide intoxication, reduced atmospheric pressure, and reduced oxygen tension [1].
In a double-blind clinical trial involving 76 healthy elderly subjects, Meclofenoxate (600 mg twice daily for 6 months) significantly improved delayed free-recall performance (P<0.01), indicating enhanced consolidation of new information into long-term memory, but did not affect immediate free-recall, digit span, recognition of famous faces, recall of past events, or prose passage memory. Post-trial questionnaire: 67% of active group reported beneficial effects (increased alertness and well-being) vs 42% of placebo group (P<0.05) [1].
In vivo, Meclofenoxate HCl has been shown to have cognitive-enhancing effects in animal models. It has been studied for its ability to improve memory and learning in rodents. The compound is also reported to have anti-aging effects, such as reducing the accumulation of lipofuscin, a pigment associated with aging. Clinical studies have investigated its use in the treatment of dementia and other cognitive disorders. Its effects are thought to be mediated through its action on the cholinergic system.
Enzyme Assay
Non-cellular assays for Meclofenoxate HCl are not typically performed, as its mechanism involves metabolic conversion and cholinergic function rather than direct enzyme inhibition. However, its stability and metabolism can be studied in biochemical systems. The compound's conversion to DMAE can be measured using analytical techniques.
Cell Assay
In vitro cell-based assays for Meclofenoxate HCl are used to study its effects on neuronal cells. These assays often involve measuring the release of acetylcholine or its precursors in cultured neurons or brain slices. Cell viability assays can be used to assess its neuroprotective effects. These studies help to elucidate its mechanism of action at the cellular level.
Animal Protocol
In vivo animal studies for Meclofenoxate HCl are standard for evaluating its cognitive-enhancing and neuroprotective effects. The compound is typically administered orally or intraperitoneally to rodents. Behavioral tests, such as the Morris water maze or passive avoidance test, are used to assess learning and memory. Brain tissue can also be analyzed for biochemical markers. These studies are crucial for validating its efficacy.
ADME/Pharmacokinetics
Meclofenoxate HCl is an orally active compound. It has a molecular weight of 294.17 g/mol. As a prodrug, it is metabolized to DMAE and p-chlorophenoxyacetic acid. Its pharmacokinetic properties have been studied in preclinical and clinical settings. It is absorbed from the gastrointestinal tract and distributed to the brain. Its half-life and bioavailability are well-characterized.
Toxicity/Toxicokinetics
Meclofenoxate HCl has an established safety profile from its clinical use. It is generally well-tolerated, with side effects such as insomnia, anxiety, and gastrointestinal disturbances reported. Comprehensive toxicological data are available from its clinical use. Meclofenoxate HCl is not a widely approved drug in many countries but has been used in some regions for cognitive disorders.
References
Age Ageing.1977 May;6(2):123-31.
Additional Infomation
An ester of dimethylaminoethanol and p-chlorophenoxyacetic acid.
Meclofenoxate is also known as Lucidril and centrophenoxine. Its chemical name is 2-dimethylaminoethyl 4-chlorophenoxyacetate hydrochloride. The drug is thought to operate through enhancement of alternative pathways of glucose metabolism (pentose shunt). In the clinical trial, untreated control subjects outperformed both treatment groups on most tests, confirming their self-rated well-being. The lack of effect on digit span (primary memory) and recognition of remote events suggests specificity for consolidation of new information. The study used a double-blind, placebo-controlled design with 9-month follow-up (6 months on medication). [1]
Meclofenoxate HCl (Centrophenoxine) is a central nervous system stimulant and cholinergic agent. It is a prodrug of dimethylaminoethanol and is used in research for its potential cognitive-enhancing and anti-aging effects. Its mechanism involves enhancing cholinergic function in the brain. Meclofenoxate HCl is not a widely approved drug and is primarily a research compound.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H17CL2NO3
Molecular Weight
294.17
Exact Mass
293.058
CAS #
3685-84-5
Related CAS #
3685-84-5
PubChem CID
19379
Appearance
White to off-white solid powder
Boiling Point
345.9ºC at 760mmHg
Melting Point
133-135°C
LogP
2.625
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
7
Heavy Atom Count
18
Complexity
228
Defined Atom Stereocenter Count
0
InChi Key
FIVHOHCAXWQPGC-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H16ClNO3.ClH/c1-14(2)7-8-16-12(15)9-17-11-5-3-10(13)4-6-11;/h3-6H,7-9H2,1-2H3;1H
Chemical Name
2-(Dimethylamino)ethyl 2-(4-chlorophenoxy)acetate hydrochloride
Synonyms

Meclofenoxate HCl; Centrophenoxine HCl; Centrophenoxine; Cerutil, Lucidril; Helfergin; Marucotol; Acefen; Atsefen; Brenal

HS Tariff Code
2934.99.9001
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, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:58 mg/mL (197.2 mM)
Water:58 mg/mL (197.2 mM)
Ethanol: N/A
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (339.94 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3994 mL 16.9970 mL 33.9939 mL
5 mM 0.6799 mL 3.3994 mL 6.7988 mL
10 mM 0.3399 mL 1.6997 mL 3.3994 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.

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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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03961087 UNKNOWN STATUS Drug:Coenzyme Q10
Drug:MECLOFENOXATE
Coenzyme Q10
Hepatic Encephalopathy
Intellectual Functioning Disability
Zagazig University 2019-05-23 Not Applicable
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