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  5. Phenytoin

Phenytoin  (Synonyms: 5,5-Diphenylhydantoin)

Cat. No.: HY-B0448 Purity: 99.91%
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Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.

For research use only. We do not sell to patients.

Phenytoin Chemical Structure

Phenytoin Chemical Structure

CAS No. : 57-41-0

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Based on 5 publication(s) in Google Scholar

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Phenytoin Related Antibodies

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  • Biological Activity

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Description

Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1][2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Phenytoin Related Antibodies
In Vivo

Phenytoin can induce a model of gingival hyperplasia in mice[6].

Induction of Gingival Hyperplasia in Mice[6]
Background
Phenytoin induced gingival overgrowth, a side effect with multifactorial aetiology, is characterized by an increase in the volume of extracellular tissues, particularly collagenous components, with varying degrees of inflammation.
Specific Mmodeling Methods
Mice: BALB/cByJ • male • 8 week old
Administration: 30 mg/kg • miniosmotic pumps • 0.5-μL/h • 2 weeks
Note
(1) Mice are housed for 1 week before any procedure for acclimation.
(2) Pumps are replaced every 2 weeks throughout the 12-week experimental period.
(3) Mice are then euthanized and heads are immediately placed in freshly made 4% paraformaldehyde for 24 hours for fixation.
Modeling Indicators
Morphology: Gingival overgrowth was apparent in the maxillary anterior gingival tissue of mice; Increased the papillary height and area.
Histomorphometry: Increased epithelial thickness and area in the maxillary anterior zone.
Molecular changes: Ccn2 is overexpressed in all regions of the epithelium; TGF-β1 and LOXL2 is overexpressed in both epithelial and connective tissues.
Correlated Product(s): Cyclosporine A (HY-B0579)
Opposite Product(s): Lovastatin (HY-N0504)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

252.27

Formula

C15H12N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(C(C2=CC=CC=C2)(C3=CC=CC=C3)N1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (198.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9640 mL 19.8200 mL 39.6401 mL
5 mM 0.7928 mL 3.9640 mL 7.9280 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

COA (258 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9640 mL 19.8200 mL 39.6401 mL 99.1002 mL
5 mM 0.7928 mL 3.9640 mL 7.9280 mL 19.8200 mL
10 mM 0.3964 mL 1.9820 mL 3.9640 mL 9.9100 mL
15 mM 0.2643 mL 1.3213 mL 2.6427 mL 6.6067 mL
20 mM 0.1982 mL 0.9910 mL 1.9820 mL 4.9550 mL
25 mM 0.1586 mL 0.7928 mL 1.5856 mL 3.9640 mL
30 mM 0.1321 mL 0.6607 mL 1.3213 mL 3.3033 mL
40 mM 0.0991 mL 0.4955 mL 0.9910 mL 2.4775 mL
50 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9820 mL
60 mM 0.0661 mL 0.3303 mL 0.6607 mL 1.6517 mL
80 mM 0.0496 mL 0.2478 mL 0.4955 mL 1.2388 mL
100 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9910 mL
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Phenytoin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Phenytoin57-41-05,5-DiphenylhydantoinSodium ChannelVirus ProteaseNa channelsNa+ channelsVoltage-gatedNa+VGSCsantiepilepticbreasttumourmetastasisInhibitorinhibitorinhibit

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