Fosphenytoin disodium
Based on 1 Customer Validation
Fosphenytoin disodium is a prodrug of Phenytoin (HY-B0448). Fosphenytoin disodium can be converted to Phenytoin in vivo, which blocks voltage-gated sodium channels in a voltage- and use-dependent manner, prolonging inactivation and slowing recovery. Fosphenytoin disodium enhances GABA responses and, at higher concentrations, mildly modulates calcium channels and increases sodium-potassium ATPase activity. Fosphenytoin disodium raises the afterdischarge threshold, reduces the severity and duration of seizures, alleviates pain-like behavior, and protects hippocampal pyramidal neurons after ischemia without altering GFAP immunoreactivity. Fosphenytoin disodium can be used in research on acute herpes zoster pain, epilepsy, and cerebral ischemia.
For research use only. We do not sell to patients.
- Purity : 99.91%
- CAS No.: 92134-98-0
- Formula: C16H13N2Na2O6P
- Molecular Weight:406.24
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
HY-B1744
Pyridoxal phosphateEndogenous Metabolite -
HY-B1829A
Dexamethasone phosphate disodiumDexamethasone Prodrug -
HY-B0703
Eslicarbazepine acetateBeta-secretase Inhibitor -
HY-B1657AR
Fosphenytoin disodium (Standard)Reference Standard -
HY-B0703R
Eslicarbazepine acetate (Standard)Beta-secretase Inhibitor
Biological Activity
Description
In Vivo
Fosphenytoin (30 mg/kg; i.m.; single injection at 5 minutes after resuscitation) disodium preserves hippocampal CA1 pyramidal neurons in rats after transient global ischemia[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (female, 6 weeks old at start, 18-20 g) bearing acute herpes zoster pain[2]
-
Dosage:15 mg/kg; 30 mg/kg
-
Administration:i.v.; single administration on day 6 after HSV-1 inoculation; before behavioral testing
-
Result:On day 6 after HSV-1 inoculation, 15 mg/kg i.v. suppressed 0.17-g mechanical allodynia at 3 h after administration; both 15 and 30 mg/kg inhibited 1.20-g mechanical hyperalgesia around 2-4 h after administration.
Table 1 reported mean differences from vehicle for the 0.17-g ipsilateral response of 0.180 (15 mg/kg) and 0.119 (30 mg/kg), and for the 1.20-g ipsilateral response of 0.405 (15 mg/kg) and 0.299 (30 mg/kg).
15 and 30 mg/kg reduced HSV-1-induced spontaneous licking in a dose-dependent manner; the 30 mg/kg dose produced the greatest numerical suppression among all trial drugs.
-
Animal Model:Wistar (female; Harlan-Winkelmann, Borchen, Germany)[4]
-
Dosage:6.25, 12.5, 25, and 50 mg/kg (Phenytoin equivalents); 10.5 mg/kg (6.25 mg/kg Phenytoin equivalent), 20.9 mg/kg (12.5 mg/kg Phenytoin equivalent), 83.5 mg/kg (50 mg/kg Phenytoin equivalent)
-
Administration:i.p.; single injection; 60 min before ADT determination
-
Result:Dose-dependently increased the ADT.
The 10.5 mg/kg dose (6.25 mg/kg phenytoin equivalent) was without effect on ADT, whereas 20.9 mg/kg (12.5 mg/kg phenytoin equivalent) increased ADT by almost 100%.
At the highest dose tested (83.5 mg/kg; 50 mg/kg phenytoin equivalent), seizure severity and seizure duration at threshold were reduced; the decrease in seizure severity was small, and generalized seizures were still seen in most rats at ADT current.
Afterdischarge duration was not changed.
Chemical Information
-
CAS No. 92134-98-0
-
Appearance Solid
-
Molecular Weight 406.24
-
Formula C16H13N2Na2O6P
-
Color White to off-white
-
SMILES
O=C1N(COP(O[Na])(O[Na])=O)C(C(C2=CC=CC=C2)(C3=CC=CC=C3)N1)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
H2O : ≥ 100 mg/mL (246.16 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (61.54 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (297 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
-
Handling Instructions (2659 KB)
References
[1]. Varia SA, et al. Phenytoin prodrugs III: water-soluble prodrugs for oral and/or parenteral use. J Pharm Sci. 1984;73(8):1068-1073. [Content Brief]
[2]. Takasaki I, et al. Fosphenytoin Alleviates Herpes Simplex Virus Infection-Induced Provoked and Spontaneous Pain-Like Behaviors in Mice. Biol Pharm Bull. 2022 Mar 1;45(3):360-363. [Content Brief]
[3]. Aleyadeh R, et al. Fosphenytoin. 2023 Aug 28. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan–. [Content Brief]
[4]. Löscher W, et al. Anticonvulsant effect of fosphenytoin in amygdala-kindled rats: comparison with phenytoin. Epilepsy Res. 1998 Mar;30(1):69-76. [Content Brief]
[5]. Chan SA, et al. Fosphenytoin reduces hippocampal neuronal damage in rat following transient global ischemia. Acta Neurochir (Wien). 1998;140(2):175-80. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.4616 mL | 12.3080 mL | 24.6160 mL | 61.5400 mL |
| 5 mM | 0.4923 mL | 2.4616 mL | 4.9232 mL | 12.3080 mL | |
| 10 mM | 0.2462 mL | 1.2308 mL | 2.4616 mL | 6.1540 mL | |
| 15 mM | 0.1641 mL | 0.8205 mL | 1.6411 mL | 4.1027 mL | |
| 20 mM | 0.1231 mL | 0.6154 mL | 1.2308 mL | 3.0770 mL | |
| 25 mM | 0.0985 mL | 0.4923 mL | 0.9846 mL | 2.4616 mL | |
| 30 mM | 0.0821 mL | 0.4103 mL | 0.8205 mL | 2.0513 mL | |
| 40 mM | 0.0615 mL | 0.3077 mL | 0.6154 mL | 1.5385 mL | |
| 50 mM | 0.0492 mL | 0.2462 mL | 0.4923 mL | 1.2308 mL | |
| 60 mM | 0.0410 mL | 0.2051 mL | 0.4103 mL | 1.0257 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3077 mL | 0.7692 mL | |
| 100 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6154 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Fosphenytoin disodium Related Classifications
HY-B1657A Related Classifications
Powered by Bioz