Retigabine dihydrochloride
(Synonyms: 瑞替加滨,D 20443 dihydrochloride;D-20443 dihydrochloride;D20443 dihydrochloride) 目录号 : GC12599
An Analytical Reference Standard
Cas No.:150812-13-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Chinese hamster ovary (CHO-K1) cells transfected with the KCNQ2/Q3 tandem construct (CHO-KCNQ2/Q3) |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
0.1 ~ 10 μM |
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Applications |
Retigabine Dihydrochloride (0.1 ~ 10 μM) induced a potassium current and hyperpolarized CHO-KCNQ2/Q3 cells but not in wild-type cells. |
| Animal experiment [2]: | |
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Animal models |
Mouse 6-Hz psychomotor seizure models |
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Dosage form |
26 or 33 mg/kg; i.p. |
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Applications |
In the 6-Hz psychomotor seizure model, Retigabine Dihydrochloride dose-dependently blocked seizures induced by either 32 or 44 mA current stimulation. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Wickenden AD, Yu W, Zou A, Jegla T, Wagoner PK. Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol Pharmacol. 2000 Sep;58(3):591-600. [2]. Large CH, Sokal DM, Nehlig A, Gunthorpe MJ, Sankar R, Crean CS, Vanlandingham KE, White HS. The spectrum of anticonvulsant efficacy of retigabine (ezogabine) in animal models: implications for clinical use. Epilepsia. 2012 Mar;53(3):425-36. |
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IC50: N/A
Retigabine is a first-in-class K+ channel (KCNQ) opener. KCNQ channels are reported to be expressed predominantly in neurons and are critical determinants of cellular excitability, as shown by the occurrence of human genetic mutations in KCNQ channels which underlie inheritable disorders including the syndrome of benign familial neonatal convulsions.
In vitro: Retigabine was found to combine a novel mode of actions, which were namely potassium channel opening (KCNQ2, KCNQ3 as well as KCNQ4 channels). Retigabine also showed activities with some potentiation of gamma amino butyric acid (GABA)-evoked currents at its higher concentrations [1].
In vivo: Animal models of epileptic seizures showed that retigabine treatment was effective at an oral dose as low as 0.01 mg/kg. Studies performed in mice also indicated that combining retigabine with another anticonvulsant agent leads to an additive effect [1].
Clinical trial: A clinical interaction study showed that there was no pharmacokinetic interaction between phenobarbitone and retigabine in healthy subjects. Thus, no dosage adjustment is likely to be necessary when phenobarbitone and retigabine are coadministered to patients [1].
Reference:
[1] Ferron GM,Patat A,Parks V,Rolan P,Troy SM. Lack of pharmacokinetic interaction between retigabine and phenobarbitone at steady-state in healthy subjects. Br J Clin Pharmacol.2003 Jul;56(1):39-45.
| Cas No. | 150812-13-8 | SDF | |
| 别名 | 瑞替加滨,D 20443 dihydrochloride;D-20443 dihydrochloride;D20443 dihydrochloride | ||
| 化学名 | ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate;dihydrochloride | ||
| Canonical SMILES | CCOC(=O)NC1=C(C=C(C=C1)NCC2=CC=C(C=C2)F)N.Cl.Cl | ||
| 分子式 | C16H20Cl2FN3O2 | 分子量 | 376.25 |
| 溶解度 | ≥ 18.8 mg/mL in DMSO, ≥ 8.71 mg/mL in EtOH with ultrasonic and warming, ≥ 52.4 mg/mL in Water with gentle warming | 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 | 2.6578 mL | 13.289 mL | 26.5781 mL |
| 5 mM | 0.5316 mL | 2.6578 mL | 5.3156 mL |
| 10 mM | 0.2658 mL | 1.3289 mL | 2.6578 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。