Mephenytoin - CAS 50-12-4
Catalog number:
50-12-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C12H14N2O2
Molecular Weight:
218.25
COA:
Inquire
Targets:
Sodium Channel
Description:
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.
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Purity:
98%
Related CAS:
70989-04-7 (s-isomer)
Appearance:
Solid powder
Synonyms:
5-ethyl-3-methyl-5-phenylimidazolidine-2,4-dione; Mephenytoin; Methoin; Mesantoin; Phenantoin; Methylphenetoin; Insulton
Solubility:
DMSO: soluble,Ethanol, Methanol
Storage:
2-8°C
MSDS:
Inquire
Application:
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
Quantity:
Grams to Kilograms
Melting Point:
136-137 °C
Density:
1.154±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
GMHKMTDVRCWUDX-UHFFFAOYSA-N
InChI:
1S/C12H14N2O2/c1-3-12(9-7-5-4-6-8-9)10(15)14(2)11(16)13-12/h4-8H,3H2,1-2H3,(H,13,16)
Canonical SMILES:
CCC1(C(=O)N(C(=O)N1)C)C2=CC=CC=C2
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.
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CAS 50-12-4 Mephenytoin

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