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Inhibitors?ScreeningLibraries?Proteins

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Teneligliptin-d5

Cat.No.:HY-14806S2

Synonyms:MP-513-d5

分?式:C??H??D?N?OS

分?量:431.61

作?靶点:Isotope-LabeledCompounds;DipeptidylPeptidase

作?通路:Others;MetabolicEnzyme/Protease

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Teneligliptin-d5(MP-513-d5)是氘代标记的Teneligliptin.Teneligliptin(MP-513)hydrobromidehydrate是

?种?服活性的和选择性的?肽基肽酶4(DPP-4)抑制剂(对?和??酶的IC50s分别为0.37和0.29nM)。

Teneligliptinhydrobromidehydrate可改善?糖?平，可?于2型糖尿病相关的研究[1][2][3][4][5][6][7]

[8]。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

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

216.

[2].YoshidaT,etal.Discoveryandpreclinicalprofileofteneligliptin(3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-

yl]pyrrolidin-2-ylcarbonyl]thiazolid