| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Valpromide targets multiple pathways. It is an inhibitor of human epoxide hydrolase. Its pharmacological effects also involve an increase in GABA levels in the brain as well as changes in membrane conductance on neurons. Valpromide modulates host enzymatic pathways and inhibits the reactivation of the Epstein-Barr virus (EBV) lytic cycle. It also exhibits antiviral activity against various viruses.
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| ln Vitro |
In vitro, valpromide (10 mM; 24-48 h) inhibits the expression of EBV lytic transactivator proteins Zebra, BZLF1, and BRLF1 in EBV-positive HH514-16 cells. It also inhibits the expression of BZLF1 and BRLF1 in EBV-infected Raji cells at 10 mM for 18 hours. Valpromide inhibits human epoxide hydrolase activity. It has been used to pretreat NIH/3T3 cells to test its effect on cytomegalovirus (CMV) viral replication.
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| ln Vivo |
In vivo, valpromide has demonstrated anticonvulsant and antipsychotic effects. In a pilocarpine rat model of focal epilepsy, valpromide (100 mg/kg) proved to be at least as effective as its parent compound sodium valproate (400 mg/kg) against pilocarpine-induced seizures. Valpromide has been shown to decrease aggressivity in stress-induced animals, regulate anxious induced behaviors, and potentiate central sedative compounds. It produces a significant increase of cognitive functions.
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| Enzyme Assay |
In vitro enzyme or receptor binding assays for valpromide involve measuring its inhibition of epoxide hydrolase activity. The assay uses purified human epoxide hydrolase or tissue homogenates and a substrate, such as styrene oxide or other epoxide substrates. The enzymatic activity is monitored by measuring the hydrolysis of the epoxide substrate using chromatographic or spectrophotometric methods. The compound is incubated with the enzyme and substrate at varying concentrations to determine inhibitory potency.
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| Cell Assay |
In vitro cell-based assays for valpromide are performed using EBV-positive cell lines such as HH514-16 and Raji cells. Cells are treated with valpromide at concentrations around 10 mM for 18-48 hours. The expression of EBV lytic transactivator proteins (Zebra, BZLF1, BRLF1) is measured by Western blotting or qPCR. Antiviral activity is assessed by measuring viral replication in CMV-infected or HSV-1 infected cells.
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| Animal Protocol |
In vivo animal experiments for valpromide are conducted using rodent models of epilepsy and behavioral disorders. In the pilocarpine rat model of focal epilepsy, valpromide is administered at 100 mg/kg. In mice of the NMRJ strain, valpromide (3 mmol/kg; subcutaneous injection; single administration on day 8 of gestation) induces a much lower rate of exencephaly (6%) compared with valproic acid. Stress-induced animal models are used to assess effects on aggressivity and anxiety.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of valpromide indicate that it is orally active and can cross the blood-brain barrier. The compound has a molecular weight of 143.23 and a molecular formula of C8H17NO. In humans, valpromide is rapidly biotransformed to valproic acid after oral administration. The bioavailability of valproic acid from valpromide is approximately 0.79-0.77 relative to a marketed tablet of valproic acid. Valpromide is soluble in DMSO at ≥50 mg/mL. Storage at room temperature for up to 3 years is recommended.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for valpromide indicate that it is much less teratogenic than valproic acid. In mice, valpromide (3 mmol/kg) induced an exencephaly rate of 6%, which was significantly higher than the control group but much lower than valproic acid. The amidation of the free carboxylic group appears to greatly decrease the teratogenic activity of valproic acid. Common side effects may include gastrointestinal disturbances, sedation, and cognitive effects.
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| References | |
| Additional Infomation |
Valproamide is a fatty amide derived from valproic acid. It is both a metabolite of valproic acid and a teratogen and anti-aging agent. Functionally, it is related to valproic acid.
Other information: Valpromide is also known as Dipropylacetamide. It is indicated for the treatment of bipolar disorder (manic episodes) and is marketed in some European countries. Psychopathological experiments have shown a wakening of personality, euphoric effects, an improvement of social behavior, and a stabilization of mood in affective disorders. Valpromide is also known as Depamide in some markets. Its CAS number is 2430-27-5. |
| Molecular Formula |
C8H17NO
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|---|---|
| Molecular Weight |
143.23
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| Exact Mass |
143.131
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| CAS # |
2430-27-5
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| PubChem CID |
71113
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| Appearance |
White to off-white solid powder
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| Density |
0.885g/cm3
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| Boiling Point |
274.6ºC at 760mmHg
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| Melting Point |
123-125°C
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| Flash Point |
119.9ºC
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| Vapour Pressure |
0.00535mmHg at 25°C
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| Index of Refraction |
1.44
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| LogP |
2.388
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
10
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| Complexity |
95.4
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OMOMUFTZPTXCHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H17NO/c1-3-5-7(6-4-2)8(9)10/h7H,3-6H2,1-2H3,(H2,9,10)
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| Chemical Name |
2-propylpentanamide
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| Synonyms |
Depamide; Valpromide
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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 |
| 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 : ≥ 50 mg/mL (~349.09 mM)
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| 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.
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