| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
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| 500mg |
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| 1g | |||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Metabolites are found only in urine. 4-Hydroxybecramite is present in higher concentrations in urine than 3-hydroxybecramite. Approximately 20% of the radiolabeled material is excreted in urine. Metabolism/Metabolites Metabolism is rapid. The main metabolic pathways are the oxidation of the benzene ring to produce 3-hydroxyphenyl and 4-hydroxyphenyl metabolites, and the oxidation of benzene methylene to produce benzoic acid. 3-hydroxyphenyl and 4-hydroxyphenyl metabolites are primarily excreted as glucuronide and sulfate conjugates, while benzoic acid is excreted as a glycine conjugate (hippuric acid). |
|---|---|
| Additional Infomation |
Beclamide belongs to the benzene class of compounds.
Beclamide (N-benzyl-β-chloropropionamide) is a discontinued drug with anticonvulsant and sedative effects. It was used in the 1950s to treat generalized tonic-clonic seizures, but was ineffective for absence seizures. Drug indications It has been used to treat epilepsy and epilepsy-related behavioral disorders. It has been used to treat generalized tonic-clonic seizures, but was ineffective for absence seizures. In recent years, research has focused on the application of Beclamide in behavioral disorders. In patients with epilepsy and intellectual disability, it has been found to reduce anxiety, antisocial behavior, compulsive behavior and impulsivity. In addition, it has been observed to have a mood-stabilizing effect. [2] Furthermore, due to its effect on monoamine neurotransmitters, Beclamide may have potential applications in the treatment of diseases such as tardive dyskinesia and ADHD. [2] Mechanism of action Beclamide has been used for more than 30 years, but little is known about its mechanism of action in the central nervous system. A rat study found that beclamitar reduced striatal dopamine and serotonin levels and increased levels of dopamine's major metabolite (thus promoting dopamine turnover), while simultaneously lowering serotonin's major metabolite levels below the detection limit. Similar changes in neurotransmitter levels were observed in the rat frontal cortex. It is theoretically suggested that aggressive behavior in animals is related to the levels of biologically derived monoamine neurotransmitters such as dopamine and serotonin, but their exact role remains unclear. |
| Molecular Formula |
C10H12NOCL
|
|---|---|
| Molecular Weight |
197.66138
|
| Exact Mass |
197.061
|
| CAS # |
501-68-8
|
| PubChem CID |
10391
|
| Appearance |
White to off-white solid powder
|
| Density |
1.145g/cm3
|
| Boiling Point |
386.9ºC at 760mmHg
|
| Flash Point |
187.8ºC
|
| Index of Refraction |
1.532
|
| LogP |
2.322
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
13
|
| Complexity |
155
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(NCC1=CC=CC=C1)CCCl
|
| InChi Key |
JPYQFYIEOUVJDU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H12ClNO/c11-7-6-10(13)12-8-9-4-2-1-3-5-9/h1-5H,6-8H2,(H,12,13)
|
| Chemical Name |
N-benzyl-3-chloropropanamide
|
| 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 |
| 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 Vitro) |
DMSO : ≥ 100 mg/mL (~505.92 mM)
H2O : ~0.67 mg/mL (~3.39 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.65 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 (12.65 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 (12.65 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 | 5.0592 mL | 25.2960 mL | 50.5919 mL | |
| 5 mM | 1.0118 mL | 5.0592 mL | 10.1184 mL | |
| 10 mM | 0.5059 mL | 2.5296 mL | 5.0592 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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