| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
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| ln Vitro |
Memantine (HCl) (D-145 (HCl)) blocks NMDA receptor chronic excess calcium influx brought on by overstimulation. It is a medium-affinity, noncompetitive, voltage-dependent NMDA receptor antagonist with fast on/off kinetics. Memantine is licensed for use in treating individuals with moderate to severe dementia of the Alzheimer's disease type in both the US and the EU [1]. Memantine exhibits significant therapeutic potential for a range of clinical conditions linked to neurotoxicity caused by NMDA receptors [2]. With an empirical Hill coefficient of roughly 1 and a 50% inhibition constant (IC50) of roughly 1 microM at -60 mV, memantine can suppress the response triggered by 200 microM NMDA [3].
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| References |
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| Additional Infomation |
Memantine hydrochloride is a hydrochloride obtained by reaction of memantine with one equivalent of hydrochloric acid. A low to moderate affinity uncompetitive (open-channel); NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels. It has a role as an antidepressant, an antiparkinson drug, a dopaminergic agent, a neuroprotective agent and a NMDA receptor antagonist. It contains a memantinium(1+).
Memantine Hydrochloride is the hydrochloride salt of memantine, a low-affinity, voltage-dependent, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist. Memantine binds to and inhibits cation channels of glutamanergic NMDA receptors located in the central nervous system (CNS), preventing the prolonged influx of calcium ions and the associated neuronal excitotoxicity, and thereby potentially enhancing cognitive function. Memantine is also a 5-hydroxytryptamine type 3 (5HT3) receptor and nicotinic receptor antagonist. AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent. See also: Memantine (has active moiety); Donepezil hydrochloride; memantine hydrochloride (component of). Drug Indication Treatment of patients with moderate to severe Alzheimer's disease. Treatment of patients with moderate to severe Alzheimer's disease. Treatment of patients with moderate to severe Alzheimer's disease Treatment of patients with moderate to severe Alzheimer's disease. Treatment of patients with moderate to severe Alzheimer's disease. Treatment of patients with moderate to severe Alzheimer's disease. Treatment of patients with moderate to severe Alzheimer's disease. Treatment of patients with moderate to severe Alzheimer's disease. Treatment of Alzheimers disease |
| Molecular Formula |
C12H21N
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|---|---|
| Molecular Weight |
179.3018
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| Exact Mass |
215.144
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| CAS # |
41100-52-1
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| Related CAS # |
Memantine-d6 hydrochloride;1189713-18-5;Memantine;19982-08-2
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| PubChem CID |
181458
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| Appearance |
White to off-white solid powder
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| Boiling Point |
239.8ºC at 760 mmHg
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| Melting Point |
292 °C
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| Flash Point |
92.3ºC
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| LogP |
4.196
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
240
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LDDHMLJTFXJGPI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H21N.ClH/c1-10-3-9-4-11(2,6-10)8-12(13,5-9)7-10;/h9H,3-8,13H2,1-2H3;1H
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| Chemical Name |
3,5-dimethyladamantan-1-amine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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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, 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~579.35 mM)
H2O : ≥ 33.33 mg/mL (~154.48 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5772 mL | 27.8862 mL | 55.7724 mL | |
| 5 mM | 1.1154 mL | 5.5772 mL | 11.1545 mL | |
| 10 mM | 0.5577 mL | 2.7886 mL | 5.5772 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01535040 | Completed | Drug: memantine hydrochloride Drug: placebo |
Breast Cancer Colorectal Cancer Lung Cancer Prostate Cancer Tobacco Use Disorder |
Wake Forest University Health Sciences | 2012-08-01 | Phase 2 |
| NCT03779672 | Completed | Drug: Memantine Hydrochloride 10 mg | Epileptic Encephalopathy, Childhood-Onset | Kenneth Myers, MD | 2019-02-07 | Phase 4 |
| NCT01333865 | Completed | Drug: Memantine | Autism Spectrum Disorders | Massachusetts General Hospital | 2010-01 | Phase 4 |
| NCT03711825 | Completed | Drug: LYN-057 Procedure: Imaging Assessment (MRI) Procedure: Imaging Assessment (U/S) |
Alzheimer Disease Gastric Retention Healthy |
Lyndra Inc. | 2018-09-10 | Early Phase 1 |
| NCT03468543 | Terminated | Drug: Memantine Hydrochloride MR Prototype Capsule Formulation A Drug: Memantine Hydrochloride MR Prototype Capsule Formulation B Drug: Memantine Hydrochloride MR Prototype Capsule Formulation C |
Gastric Retention Healthy |
Lyndra Inc. | 2017-07-26 | Early Phase 1 |
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