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文件名称:Telcagepant-d8-MK-0974-d-sub-8-sub-生命科学试剂-MCE.pdf
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文档摘要

Hotline:400-820-3792

Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Telcagepant-d8

Cat.No.:HY-32709S

CASNo.:1132641-75-8

Synonyms:MK-0974-d8

分?式:C??H??D?F?N?O?

分?量:574.57

作?靶点:Isotope-LabeledCompounds;CGRPReceptor

作?通路:Others;GPCR/GProtein;NeuronalSignaling

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Telcagepant-d8(MK-0974-d8)是氘代标记的Telcagepant.Telcagepant(MK-0974)是?种?服有效的降钙素

基因相关肽(CGRP)受体拮抗剂,与?和恒河猴CGRP结合的Ki分别为0.77nM和1.2nM。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

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

216.

[2].RollerS,etal.PreclinicalpharmacokineticsofMK-