Valrocemide (Synonyms: N-Valproyl glycinamide, TV1901, VGD) |
Catalog No.GC17434
One-Click Copy Product Info
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anticonvulsant agent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 92262-58-3
Sample solution is provided at 25 µL, 10mM.
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Epilepsy is a chronic condition requiring long-term drug treatment, often for the patient's entire life. Valrocemide is an anticonvulsant agent under development by Teva and Acorda as a therapeutic for the treatment of epilepsy.
In vitro: It was found that 1 mM of valrocemide could drastically inhibit human brain crude homogenate MIP synthase activity. Furthermore, the mechanism of the effect of valrocemide were studied and results showed that valrocemide reduced the enzyme activity by an apparent competitive mode of inhibition [1].
In vivo: In mice, valrocemide showed complete protection against maximal electroshock-, pentylenetetrazole-, picrotoxin-, bicuculline-induced seizures as well as 6-Hz "psychomotor" seizures with ED50 values of 151, 132, 275, 248, and 237 mg/kg, respectively. Valrocemide was also effective in preventing sound-induced seizures in Frings audiogenic-seizure susceptible mice. The neurotoxic dose in mice was 332 mg/kg. After oral administration to rats, valrocemide was active in the maximal electroshock test, with an ED50 of 73 mg/kg, and the median neurotoxic dose was 1,000 mg/kg. IP administration of 300 mg/kg of valrocemide to hippocampal kindled SD rats blocked generalized seizures and shortened the afterdischarge duration significantly. Valrocemide also had complete protection from focal seizures in the corneally kindled rats [2].
Clinical trial: Valrocemide is a new antiepileptic drug currently undergoing phase II clinical trials in patients with refractory epilepsy [2].
References:
[1] Shaltiel G,Mark S,Kofman O,Belmaker RH,Agam G. Effect of valproate derivatives on human brain myo-inositol-1-phosphate (MIP) synthase activity and amphetamine-induced rearing. Pharmacol Rep.2007 Jul-Aug;59(4):402-7.
[2] Isoherranen N,Woodhead JH,White HS,Bialer M. Anticonvulsant profile of valrocemide (TV1901): a new antiepileptic drug. Epilepsia.2001 Jul;42(7):831-6.
Animal experiment: | Rats: Effect of valrocemide on the afterdischarge threshold in hippocampal kindled rats is evaluated in rats kindled according to this procedure. On the day of the test, the individual rat's afterdischarge threshold is determined by increasing the current intensity stepwise until the rat displayed an electrographic afterdischarge with duration of 4 s. For afterdischarge threshold determination, the initial stimulation is conducted at 20 μA and increased in 10-μA increments every 1–2 min until an afterdischarge is elicited. After administration of valrocemide, the individual rat's afterdischarge threshold is redetermined at times 0.5, 1, 2, and 4 h; ADD and BSS are recorded at each time point and compared with the control values obtained before drug administration. The criteria for seizure scoring is as described earlier for corneally kindled animals[1]. Mice: The intravenous (i.v.) pentylenetetrazole seizure threshold test (i.v. Met) also is used. At the TPE of valrocemide, infusion (0.34 ml/min) of 0.15% heparinized solution of pentylenetetrazole (0.5%) is started into the tail vein of a mouse, and the times to the appearance of the first myoclonic jerk and the subsequent sustained clonic seizure are recorded. A group of 10 drug-treated (132 mg/kg valrocemide, i.p.) mice is compared with 10 vehicle-treated controls. The time is converted to the dose of pentylenetetrazole in mg/kg. The i.v. Met test is performed according to the same procedure also after prolonged administration of valrocemide daily, i.p. (132 mg/kg) for 5 consecutive days[1]. |
References: [1]. Isoherranen N, et al. Anticonvulsant profile of valrocemide (TV1901): a new antiepileptic drug. Epilepsia. 2001 Jul;42(7):831-6. | |
| Cas No. | 92262-58-3 | SDF | |
| Synonyms | N-Valproyl glycinamide, TV1901, VGD | ||
| Chemical Name | N-(2-amino-2-oxoethyl)-2-propylpentanamide | ||
| Canonical SMILES | CCCC(CCC)C(NCC(N)=O)=O | ||
| Formula | C10H20N2O2 | M.Wt | 200.28 |
| Solubility | ≥ 20mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.993 mL | 24.965 mL | 49.9301 mL |
| 5 mM | 998.6 μL | 4.993 mL | 9.986 mL |
| 10 mM | 499.3 μL | 2.4965 mL | 4.993 mL |
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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)