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文件名称：Lomitapide-d4-AEGR-733-d-sub-4-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

Lomitapide-d4

Cat.No.:HY-14667S1

CASNo.:857296-42-5

Synonyms:AEGR-733-d;BMS-201038-d

44

分?式:C??H??D?F?N?O?

分?量:697.75

作?靶点:Isotope-LabeledCompounds;MicrosomalTriglyceride

TransferProtein(MTP)

作?通路:Others;MetabolicEnzyme/Protease

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Lomitapide-d4(AEGR-733-d4)是氘代标记的Lomitapide.Lomitapide(AEGR-733;BMS-201038)是?效的微

粒体?油三酯转移蛋?(MTP)抑制剂，体内试验的IC50值为8nM。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsof