Phenytoin (5,5-Diphenylhydantoin) 是一种有效的电压门控 Na+通道 (VGSCs) 阻滞剂。Phenytoin 具有抗癫痫活性,也可减少小鼠乳腺肿瘤的生长和转移。
生物活性 | Phenytoin (5,5-Diphenylhydantoin) is a potentVoltage-gated Na+channels (VGSCs)blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1][2]. |
体外研究 (In Vitro) | Phenytoin is an antiepileptic drug. It is useful to partial seizures and generalized tonic-clonic seizures but not primary generalized seizures such as absence seizures or myoclonic seizures. Phenytoin is believed to protect against seizures by causing voltage-dependent block of voltage-gated sodium channels[2]. Phenytoin has low affinity for resting sodium channels at hyperpolarized membrane potentials[3]. When neurons are depolarized and the channels transition into the open and inactivated states, greater binding and block occur. The inhibitory potency is strongly use dependent, so that block accumulates with prolonged or repetitive activation, such as occurs during a seizure discharge. The blocking of sodium channels by phenytoin is of slow onset. The time course of fast sodium currents is therefore not altered in the presence of the drug and action potentials evoked by synaptic depolarizations of ordinary duration are not blocked. Thus phenytoin is able to selectively inhibit pathological hyperexcitability in epilepsy without unduly impairing ongoing activity. Phenytoin also blocks persistent sodium current and this may be of particular importance in seizure control. Phenytoin is a class 1b antiarrhythmic[4].
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体内研究 (In Vivo) | Phenytoin (5,5-Diphenylhydantoin; 60 mg/kg; daily; 28 days ) reduces tumour growth in six week-old female Rag2-/-Il2rg-/-mice with MDA-MB-231 cells[1].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(198.20 mM;Need ultrasonic) 配制储备液 1 mM | 3.9640 mL | 19.8200 mL | 39.6401 mL | 5 mM | 0.7928 mL | 3.9640 mL | 7.9280 mL | 10 mM | 0.3964 mL | 1.9820 mL | 3.9640 mL |
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以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (9.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.91 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.91 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (9.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.91 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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