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文件名称:Mexiletine-d6-KOE-1173-d-sub-6-sub-生命科学试剂-MCE.pdf
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文档摘要

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Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Mexiletine-d6

Cat.No.:HY-119521S1

CASNo.:1330267-50-9

Synonyms:KOE-1173-d6

分?式:C??H??D?NO

分?量:185.3

作?靶点:Isotope-LabeledCompounds;SodiumChannel

作?通路:Others;MembraneTransporter/IonChannel

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Mexiletine-d6(KOE-1173-d6)是氘代标记的Mexiletine.Mexiletine是?种?服有效的抗?律失常剂,也被发

现对肌强直和神经病理性疼痛有效。Mexiletine通过阻断钠离?通道(IC50:75±8μM于封闭性阻断,

23.6±2.8μM于使?依赖性阻断)发挥作?,可被?于??管与神经病学研究[1][2][3][4][5]。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019;53(2):211-

216