Mephenytoin - CAS 50-12-4
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Sodium Channel
Mephenytoin is known to target sodium channel protein type 5 subunit alpha. It is a hydantoin-derivative anticonvulsant used to control various partial seizures. It may cause blood dyscrasias. It is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. It can be used to screen for such mutations by assaying its metabolites in urine. It is still studied largely because of its interesting hydroxylation polymorphism. It has been listed.
Publictions citing BOC Sciences Products
  • >> More
Related CAS:
70989-04-7 (s-isomer)
Solid powder
5-ethyl-3-methyl-5-phenylimidazolidine-2,4-dione; Mephenytoin; Methoin; Mesantoin; Phenantoin; Methylphenetoin; Insulton
DMSO: soluble,Ethanol, Methanol
Mephenytoin is used to control various partial seizures. It may cause blood dyscrasias. It can be used to screen for such mutations by assaying its metabolites in urine.
Quality Standard:
In-house standard
Grams to Kilograms
Melting Point:
136-137 °C
1.154±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
Canonical SMILES:
Current Developer:
Mephenytoin has been listed.
1.Sodium tanshinone IIA sulfonate and its interactions with human CYP450s.
Chen D1, Lin XX1, Huang WH1, Zhang W1, Tan ZR1, Peng JB1, Wang YC2, Guo Y2, Hu DL2, Chen Y1,2. Xenobiotica. 2016 Mar 2:1-8. [Epub ahead of print]
1.Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA, a famous Chinese medicine used for many years to treat cardiovascular disorders. However, the role of cytochrome P450 (CYP) enzymes in the metabolism of STS was unclear. In this study, we screened the main CYPs for the metabolism of STS and studied their interactions in vitro. 2.Seven CYPs were screened for the metabolism of STS by human liver microsomes (HLMs) or recombinant CYP isoforms. To determine the potential of STS to affect CYP-mediated phase I metabolism in humans, phenacetin (CYP1A2), coumarin (CYP2A6), tolbutamide (CYP2C9), metoprolol (CYP2D6), chlorzoxazone (CYP2E1), S-Mephenytoin (CYP2C19), and midazolam (CYP3A4) were used as the respective probe substrates. Enzyme kinetic studies were performed to investigate the mode of inhibition of the enzyme-substrate interactions. 3.STS inhibited the activity of CYP3A4 in a dose-dependent manner in the HLMs and CYP3A4 isoform.
2.Simultaneous Screening of Activities of Five Cytochrome P450 and Four Uridine 5'-Diphospho-glucuronosyltransferase Enzymes in Human Liver Microsomes Using Cocktail Incubation and Liquid Chromatography-Tandem Mass Spectrometry.
Lee B1, Ji HK1, Lee T1, Liu KH2. Drug Metab Dispos. 2015 Jul;43(7):1137-46. doi: 10.1124/dmd.114.063016. Epub 2015 Apr 22.
Cytochrome P450 (P450) and uridine 5'-diphospho-glucuronosyltransferase (UGT) are major metabolizing enzymes in the biotransformation of most drugs. Altered P450 and UGT activities are a potential cause of adverse drug-drug interaction. A method for the simultaneous evaluation of the activities of five P450s (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A) and four UGTs (UGT1A1, UGT1A4, UGT1A9, and UGT2B7) was developed using in vitro cocktail incubation and tandem mass spectrometry. The nine probe substrates used in this assay were phenacetin (CYP1A2), diclofenac (CYP2C9), S-mephenytoin (CYP2C19), dextromethorphan (CYP2D6), midazolam (CYP3A), 7-ethyl-10-hydroxy-camptothecin (SN-38) (UGT1A1), trifluoperazine (UGT1A4), mycophenolic acid (UGT1A9), and naloxone (UGT2B7). This new method involves incubation of two cocktail doses and single cassette analysis. The two cocktail doses and the concentration of each probe substrate in vitro were determined to minimize mutual drug interactions among substrates.
3.A comprehensive assay for nine major cytochrome P450 enzymes activities with 16 probe reactions on human liver microsomes by a single LC/MS/MS run to support reliable in vitro inhibitory drug-drug interaction evaluation.
Peng Y1, Wu H1, Zhang X1, Zhang F1, Qi H1, Zhong Y1, Wang Y1, Sang H1, Wang G1, Sun J1. Xenobiotica. 2015;45(11):961-77. doi: 10.3109/00498254.2015.1036954. Epub 2015 May 26.
1. A comprehensive method for the simultaneous characterization of xenobiotic compound inhibition of nine major CYP enzymes in human liver microsomes was established by using 16 CYP-catalyzed reactions of 14 probe substrates with three cocktail incubation sets and a single LC/MS/MS analysis. 2. The three cocktail subgroups were developed to minimize the effects of organic solvents, polyunsaturated fatty acids and mutual substrate interactions: Group I was composed of tolbutamide (CYP2C9), S-mephenytoin (CYP2C19), testosterone (CYP3A4), dextromethorphan (CYP2D6); Group II was composed of nifedipine (CYP3A4), midazolam (CYP3A4), coumarin (CYP2A6), bupropion (CYP2B6), diclofenac (CYP2C9); Group III was composed of phenacetin (CYP1A2), chlorzoxazone (CYP2E1), omeprazole (CYP2C19 and CYP3A4), paclitaxel (CYP2C8), (+)-bufuralol (CYP2D6). In the case of CYP2C9, CYP2C19, CYP2D6 and CYP3A4, multiple probe substrates were used due to the phenomenon of multiple substrate-binding pockets and substrate-dependent inhibition.
4.In vitro functional analysis of 24 novel CYP2C19 variants recently found in the Chinese Han population.
Dai DP1, Hu LM2, Geng PW3, Wang SH3, Cai J1,4, Hu GX4, Cai JP1. Xenobiotica. 2015;45(11):1030-5. doi: 10.3109/00498254.2015.1028512. Epub 2015 Jul 7.
1. CYP2C19 is a highly polymorphic enzyme responsible for the metabolism of a wide range of clinical drugs. Alterations to the CYP2C19 gene contribute to the variability of CYP2C19 enzyme activity, which causes pharmacokinetics and drug efficacies to vary and adverse drug reactions to occur in different persons. Recently, we identified 24 novel CYP2C19 allelic variants in the Chinese Han population. The purpose of present study is to assess the impact of these newly found nucleotide mutations on the enzymatic activity of the CYP2C19 protein. 2. Dual-expression vectors were constructed and transiently transfected into 293FT cells. Forty-eight hours after transfection, cells were re-suspended and incubated with two typical probe substrates, omeprazole and S-mephenytoin, to determine the activities of each variant relative to the wild-type protein. 3. Immunoblotting results showed that the protein expression levels of the CYP2C19 variants were diverse.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Sodium Channel Products

CAS 34183-22-7 Propafenone hydrochloride

Propafenone hydrochloride
(CAS: 34183-22-7)

Propafenone is a Class 1C antiarrhythmic as sodium channel blocker by slowing the influx of sodium ions into the cardiac muscle cells.

Sodium Channel inhibitor 1
(CAS: 1198117-23-5)

Sodium Channel inhibitor 1, a 3-Oxoisoindoline-1-carboxamide derivative, is an effective voltage-gated sodium channel blocker that could be used for pain treatm...

(CAS: 1092977-61-1)

Evenamide is a selective voltage-gated sodium and​/or calcium channel modulator, including subtypes Nav1.3, Nav1.7, and Nav1.8. It may be potentia useful in pre...

CAS 22059-60-5 Disopyramide phosphate

Disopyramide phosphate
(CAS: 22059-60-5)

Disopyramide phosphate is an oral antiarrhythmic agent for the treatment of cardiac arrhythmias. Disopyramide is a sodium channel blocker and therefore classifi...

CAS 166196-11-8 CGP-47292

(CAS: 166196-11-8)

CGP-47292, a triazole compound, has been found to be a metabolite of CGP-33101 that could be used agaist Lennox-Gastaut syndrome as a Sodium Channel antagonist.

CAS 5370-01-4 Mexiletine Hydrochloride

Mexiletine Hydrochloride
(CAS: 5370-01-4)

Mexiletine HCl belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.

CAS 2609-46-3 Amiloride

(CAS: 2609-46-3)

Amiloride, a pyrazine derivative potassium-sparing diuretic, is a blocker of sodium channel in renal epithelial cells. Amiloride blocked the low threshold Ca2+ ...

CAS 6108-05-0 Lidocaine hydrochloride monohydrate

Lidocaine hydrochloride monohydrate
(CAS: 6108-05-0)

Lidocaine hydrochloride monohydrate is the hydrochloride monohydrate form of lidocaine, which is an aminoethylamide and a prototypical member of the amide class...

CAS 892546-37-1 PH-064

(CAS: 892546-37-1)

PH-064 is a sodium channel inhibitor. It is extracted from patent FR 2879460 A1.

(CAS: 1235403-62-9)

PF-05089771, a Nav1.7 channel blocker, has been studied to have potential effect in the treatment of chronic neuropathic pain. It is still under Phase II clinic...

CAS 550-83-4 Propoxycaine hydrochloride

Propoxycaine hydrochloride
(CAS: 550-83-4)

Propoxycaine hydrochloride is the hydrochloride salt form of Propoxycaine used to control the pain of intramuscular injection of penicillin as well as in dentis...

(CAS: 1262618-39-2)

GS967, also known as GS-458967, is a highly selective late sodium channel current blocker. The selective inhibition of late INa with GS967 can exert antiarrhyth...

(CAS: 1332295-35-8)

Nav1.7-IN-2, a voltage-gated sodium channels, could be probably effective in chronic pain therapy. IC50: 80 nM.

(CAS: 199467-52-2)

AM-36 is a potent blocker of batrachotoxinin (BTX)-sensitive Na+ channel binding in rat brain homogenates with an IC50 of 0.28 microM. As a unique neuroprotecti...

CAS 536-43-6 Dyclonine Hydrochloride

Dyclonine Hydrochloride
(CAS: 536-43-6)

Dyclonine HCl is a hydrochloride salt form of dyclonine which is an oral anaesthetic.

CAS 31883-05-3 Moricizine

(CAS: 31883-05-3)

Moricizine, a Phenothiazine derivative, is effective in suppressing premature ventricular contractions, couplets, and nonsustained ventricular tachycardia. And ...

CAS 61-12-1 Dibucaine Hydrochloride

Dibucaine Hydrochloride
(CAS: 61-12-1)

Dibucaine HCl is a local anesthetics.Among the most potent and toxic of the long-acting local anesthetics, current use of it is generally restricted to spinal a...

CAS 132112-35-7 Ropivacaine Hydrochloride

Ropivacaine Hydrochloride
(CAS: 132112-35-7)

Ropivacaine hydrochloride is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

CAS 212778-82-0 Elpetrigine

(CAS: 212778-82-0)

Elpetrigine, also known as GW 273293 and JZP-4, has a blocking effect on calcium channels and potassium channels which has been in clinical bipolar disorders an...

(CAS: 313254-51-2)

ICA-121431 is a potent and selective inhibitor of human NaV1.3 (IC50=13 nM) and NaV1.1 channels (IC50=23 nM) with 1,000 fold selectivity against other resistant...

Chemical Structure

CAS 50-12-4 Mephenytoin

Quick Inquiry

Verification code

Featured Items