| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Valnoctamide acts directly on GABAA receptors, enhancing the inhibitory effect of GABA. It enhances phasic inhibition, making it a potential target for the treatment of benzodiazepine-refractory status epilepticus. Valnoctamide is a derivative of valproate and has antiepileptic and anticonvulsant effects. It also inhibits acyl-CoA synthetase 4 (Acsl4), which is involved in arachidonic acid metabolism.
|
|---|---|
| ln Vitro |
In vitro, Valnoctamide acts directly on GABAA receptors. It enhances phasic inhibition. Its in vitro activity is characterized by potentiation of GABAergic signaling. Valnoctamide has been shown to have stronger antiepileptic effects than valproic acid in various animal models. It exhibits analgesic effects in neuropathic pain models.
|
| ln Vivo |
In vivo, Valnoctamide suppresses benzodiazepine-refractory status epilepticus. It has antiepileptic and anticonvulsant effects in various animal models. Valnoctamide also exhibits analgesic effects in neuropathic pain models. It enhances the inhibitory effect of GABA in the brain. Its in vivo efficacy is attributed to its action on GABAA receptors.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Valnoctamide typically involve measuring its binding to GABAA receptors. The compound acts directly on GABAA receptors. These assays confirm its mechanism of action as a GABAA receptor modulator. Its effects on GABA-mediated chloride currents can also be assessed using electrophysiological techniques.
|
| Cell Assay |
In vitro cellular assays for Valnoctamide typically involve studying its effects on GABAergic signaling in neuronal cultures. The compound enhances the inhibitory effect of GABA. These cell-based studies demonstrate its potentiation of GABAergic neurotransmission. Its effects on neuronal excitability can also be assessed using electrophysiological recordings.
|
| Animal Protocol |
In vivo animal models for Valnoctamide include models of epilepsy and neuropathic pain. Valnoctamide suppresses benzodiazepine-refractory status epilepticus and has antiepileptic effects in various animal models. It exhibits analgesic effects in neuropathic pain models. Doses and administration routes are optimized based on the specific model and experimental endpoints.
|
| ADME/Pharmacokinetics |
Valnoctamide has a molecular weight of 143.23 and a molecular formula of C8H17NO. Its CAS number is 4171-13-5. The compound is also known as Valmethamide. It is a derivative of valproate and acts directly on GABAA receptors. Valnoctamide suppresses benzodiazepine-refractory status epilepticus and has antiepileptic and anticonvulsant effects.
|
| Toxicity/Toxicokinetics |
Valnoctamide is a GABAA receptor modulator with a well-characterized mechanism of action. As with any GABAergic drug, potential toxicity may include sedation, dizziness, and cognitive impairment. The compound's safety profile should be evaluated in preclinical toxicology studies. Valnoctamide is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying GABAergic signaling and epilepsy.
|
| References | |
| Additional Infomation |
Valnoctamide is a fatty amide. Valnoctamide has been used in trials investigating its use for the treatment of mania and schizoaffective disorder (manic type).
Valnoctamide (CAS# 4171-13-5), also known as Valmethamide, is a derivative of valproate that acts directly on GABAA receptors. It suppresses benzodiazepine-refractory status epilepticus and enhances the inhibitory effect of GABA. Valnoctamide has antiepileptic and analgesic effects in animal models. The compound is for research use only and not for human therapeutic use. |
| Molecular Formula |
C8H17NO
|
|---|---|
| Molecular Weight |
143.23
|
| Exact Mass |
143.131
|
| CAS # |
4171-13-5
|
| Related CAS # |
Valnoctamide-d5;1190015-82-7
|
| PubChem CID |
20140
|
| Appearance |
White to light brown solid powder
|
| Density |
0.883g/cm3
|
| Boiling Point |
274.4ºC at 760mmHg
|
| Melting Point |
113.5-114ºC
|
| Flash Point |
119.8ºC
|
| Index of Refraction |
1.438
|
| LogP |
2.244
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
10
|
| Complexity |
112
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
QRCJOCOSPZMDJY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C8H17NO/c1-4-6(3)7(5-2)8(9)10/h6-7H,4-5H2,1-3H3,(H2,9,10)
|
| Chemical Name |
2-ethyl-3-methylpentanamide
|
| Synonyms |
MI-181 MI181 Valnoctamide
|
| 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 (~698.18 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (17.45 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 (17.45 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 (17.45 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 | 6.9818 mL | 34.9089 mL | 69.8178 mL | |
| 5 mM | 1.3964 mL | 6.9818 mL | 13.9636 mL | |
| 10 mM | 0.6982 mL | 3.4909 mL | 6.9818 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
