Valrocemide
(Synonyms: 丙戊塞胺; TV1901) 目录号 : GC17434
An anticonvulsant
Cas No.:92262-58-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| Cas No. | 92262-58-3 | SDF | |
| 别名 | 丙戊塞胺; TV1901 | ||
| 化学名 | N-(2-amino-2-oxoethyl)-2-propylpentanamide | ||
| Canonical SMILES | CCCC(CCC)C(NCC(N)=O)=O | ||
| 分子式 | C10H20N2O2 | 分子量 | 200.28 |
| 溶解度 | ≥ 20mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.993 mL | 24.965 mL | 49.9301 mL |
| 5 mM | 0.9986 mL | 4.993 mL | 9.986 mL |
| 10 mM | 0.4993 mL | 2.4965 mL | 4.993 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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