Fosphenytoin disodium
(Synonyms: 磷苯妥英钠) 目录号 : GC33678A prodrug of phenytoin
Cas No.:92134-98-0
Sample solution is provided at 25 µL, 10mM.
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Fosphenytoin is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker, in vivo.1,2,3 It induces less tissue damage compared with two other phenytoin prodrugs in rats following subcutaneous and intramuscular administration.1 Fosphenytoin has anticonvulsant activity in a mouse model of maximal electroshock seizures similar to that of phenytoin (ED50s = 16 and 8 mg/kg, respectively).2 It also has antiarrhythmic activity in isolated guinea pig atria and in anesthetized dogs. Formulations containing fosphenytoin have been used in the treatment of status epilepticus.
1.Varia, S.A., and Stella, V.J.Phenytoin prodrugs VI: In vivo evaluation of a phosphate ester prodrug of phenytoin after parenteral administration to ratsJ. Pharm. Sci.73(8)1087-1090(1984) 2.Smith, R.D., Brown, B.S., Maher, R.W., et al.Pharmacology of ACC-9653 (phenytoin prodrug)Epilepsia30(Suppl. 2)S15-S21(1989) 3.Boucher, B.A.Fosphenytoin: A novel phenytoin prodrugPharmacotherapy16(5)777-791(1996)
Animal experiment: | A total of four groups of rats, including normal (n=2), sham operated (n=2), ischemia with saline-treated (n=2), and ischemia with fosphenytoin-treated (n=2), are studied. Postischemic rats in saline-treated and fosphenytoin-treated groups receive a single i.m. injection of saline or fosphenytoin (30 mg/kg), respectively, in the right hind limb 5 minutes after resuscitation. Sham-operated animals are treated similarly except for chest compression. All rats are killed on the 7th postischemic day by decapitation. Brains are immediately removed, bisected longitudinally, and immersed in 4% buffered neutral formaldehyde containing 0.25% glutaraldehyde for a minimum of 2 days at 4°C. Portions of the brain containing the dorsal hippocampus are coronally sectioned with a vibratome at 40 μm. With the aid of a dissecting microscope, rectangular blocks of about 1 mm2 in size encompassing the mid-CA1 region from sections that approximate Bregma -3.6 are dissected, postfixed in 2% osmium tetroxide, and dehydrated in ascending concentrations of ethanol before being embedded in Araldite 502. Sections of polymerized blocks 1 μm thick are cut and toluidine blue stained for light microscopic examination. |
References: [1]. Chan SA, et al. Fosphenytoin reduces hippocampal neuronal damage in rat following transient global ischemia. Acta Neurochir (Wien). 1998;140(2):175-80. | |
| Cas No. | 92134-98-0 | SDF | |
| 别名 | 磷苯妥英钠 | ||
| Canonical SMILES | O=C1N(COP([O-])([O-])=O)C(C(C2=CC=CC=C2)(C3=CC=CC=C3)N1)=O.[Na+].[Na+] | ||
| 分子式 | C16H13N2Na2O6P | 分子量 | 406.24 |
| 溶解度 | Water : ≥ 100 mg/mL (246.16 mM) | 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 | 2.4616 mL | 12.308 mL | 24.616 mL |
| 5 mM | 0.4923 mL | 2.4616 mL | 4.9232 mL |
| 10 mM | 0.2462 mL | 1.2308 mL | 2.4616 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet