| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
NMDA receptor (inhibitor) and GABAA receptor (modulator). Felbamate-d4 is the deuterated form of Felbamate, an antiepileptic drug that inhibits NMDA receptors and modulates GABAA receptors.
|
|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Felbamate, the unlabeled form, is an antiepileptic drug that acts as an inhibitor of NMDA receptors and a modulator of GABAA receptors. It has broad-spectrum inhibitory activity against excitatory amino acid receptors. The deuterated form, Felbamate-d4, is expected to exhibit identical pharmacological properties due to the minimal isotopic effect of deuterium substitution. |
| ln Vivo |
In vivo, Felbamate is used clinically as an antiepileptic drug for the treatment of seizures. It exerts its anticonvulsant effects through its actions on NMDA and GABAA receptors. Felbamate-d4 is used as an internal standard in pharmacokinetic studies to accurately measure the concentration of Felbamate in biological samples.
|
| Enzyme Assay |
In vitro receptor binding assays for Felbamate are performed to evaluate its affinity for NMDA and GABAA receptors. Radioligand binding studies using membrane preparations from brain tissue or cells expressing the target receptors are conducted. The compound's ability to displace specific radiolabeled ligands is measured to calculate its binding affinities. Functional assays are used to confirm its inhibitory and modulatory activities.
|
| Cell Assay |
In vitro cell-based assays are conducted using neurons or cell lines expressing NMDA or GABAA receptors. The cells are treated with Felbamate, and receptor activity is measured by assessing downstream signaling events such as calcium mobilization or chloride influx. The compound's ability to modulate these receptors is quantified.
|
| Animal Protocol |
In vivo animal studies for Felbamate are conducted to evaluate its anticonvulsant activity. The compound is typically administered orally or via intraperitoneal injection. Its effects on seizure activity are assessed in various seizure models, such as the maximal electroshock seizure (MES) test or the pentylenetetrazole (PTZ) test. Felbamate-d4 is used as an internal standard in these studies for pharmacokinetic analysis.
|
| ADME/Pharmacokinetics |
Felbamate-d4 is used as an internal standard for the quantification of felbamate in biological matrices using mass spectrometry. As a deuterated compound, it exhibits practically identical chemical properties to unlabeled Felbamate, making it an ideal internal standard. Its use improves the accuracy and precision of analytical methods by correcting for variations in sample preparation, injection volume, and ionization efficiency.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for Felbamate-d4. As a deuterated form of Felbamate, its toxicity profile is expected to be similar to that of unlabeled Felbamate. Felbamate is associated with serious adverse effects, including aplastic anemia and hepatotoxicity, which have limited its clinical use.
|
| References |
|
| Additional Infomation |
Felbamate-d4 is the deuterium-labeled form of Felbamate, an antiepileptic drug that inhibits NMDA receptors and modulates GABAA receptors. It is intended for use as an internal standard for the quantification of felbamate by GC- or LC-MS. The compound is not intended for human therapeutic use and is strictly for research purposes.
|
| Molecular Formula |
C11H10D4N2O4
|
|---|---|
| Molecular Weight |
242.26
|
| Exact Mass |
242.12
|
| CAS # |
106817-52-1
|
| Related CAS # |
Felbamate;25451-15-4
|
| PubChem CID |
13620359
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.361
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
17
|
| Complexity |
246
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H]C([2H])(C(C1=CC=CC=C1)C([2H])([2H])OC(=O)N)OC(=O)N
|
| InChi Key |
WKGXYQFOCVYPAC-KXGHAPEVSA-N
|
| InChi Code |
InChI=1S/C11H14N2O4/c12-10(14)16-6-9(7-17-11(13)15)8-4-2-1-3-5-8/h1-5,9H,6-7H2,(H2,12,14)(H2,13,15)/i6D2,7D2
|
| Chemical Name |
(3-carbamoyloxy-1,1,3,3-tetradeuterio-2-phenylpropyl) carbamate
|
| 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 (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 | 4.1278 mL | 20.6390 mL | 41.2780 mL | |
| 5 mM | 0.8256 mL | 4.1278 mL | 8.2556 mL | |
| 10 mM | 0.4128 mL | 2.0639 mL | 4.1278 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
