K777-tosylate-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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K777tosylate

Cat.No.:HY-119293A

CASNo.:502960-91-0

分⼦式:C₃₉H₄₆N₄O₇S₂

分⼦量:746.94

作⽤靶点:Cathepsin;CCR;CytochromeP450;Parasite;SARS-CoV;

Filovirus

作⽤通路:MetabolicEnzyme/Protease;GPCR/GProtein;

Immunology/Inflammation;Anti-infection

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性K777tosylate是⼀种有效的，⼝服活性且不可逆的半胱氨酸蛋⽩酶(cysteineprotease)抑制剂，也是⼀种有

效的CYP3A4抑制剂，IC50为60nM，是⼀种选择性的CCR4拮抗剂，具有强的趋化性抑制作⽤。K777

tosylate不可逆地抑制锥⾍（克鲁斯锥⾍的主要半胱氨酸蛋⽩酶）和组织蛋⽩酶B和L。K777tosylate是⼀种

⼴谱抗病毒活性分⼦，通过靶向组织蛋⽩酶介导的细胞进⼊。K777tosylate抑制SARS-CoV和EBOV病毒的进

⼊，IC50值分别为0.68nM和0.87nM。

客户使⽤本产品发表的科研⽂献

•bioRxiv.2023Nov5.

Seemorecustomervalidationsonwww.MedChemE

REFERENCES

[1].ZhouY,etal.Proteaseinhibitorstargetingcoronavirusandfilovirusentry.AntiviralRes.2015Apr;116:76-84.

[2].JacobsenW,etal.InvitroevaluationofthedispositionofAnovelcysteineproteaseinhibitor.DrugMetabDispos.2000

Nov;28(11):1343-51.

[3].SatoT,etal.InternalizationofCCR4andinhibitionofchemotaxisbyK777,apotentandselectiveCCR4antagonist.Pharmacology.

2013;91(5-6):305-13.

[4].NdaoM,etal.Acysteinepr