Fandosentan-potassium-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

Fandosentanpotassium

Cat.No.:HY-105408A

CASNo.:221246-12-4

分⼦式:C₂₅H₁₇F₃KNO₆S

分⼦量:555.56

作⽤靶点:EndothelinReceptor;CytochromeP450

作⽤通路:GPCR/GProtein;MetabolicEnzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Fandosentanpotassium是⼀种强效的内⽪素A受体(ETAR)拮抗剂。Fandosentanpotassium可抑制

CYP2C9和CYP3A4活性,IC50值分别为39.6μM和21.6μM。Fandosentanpotassium在新⽣羔⽺模型中

,能够逆转缺氧引起的肺⾎管收缩。Fandosentanpotassium可⽤于肺动脉⾼压的研究[1][2]。

IC50TargetCYP3A4CYP2C9

21.6μM(IC50)39.6μM(IC50)

REFERENCES

[1].SahiJ,etal.Metabolismandtransporter-mediateddrug-druginteractionsoftheendothelin-AreceptorantagonistCI-1034.ChemBiol

Interact.2006Feb1;159(2):156-68.

[2].CoeY,etal.TheendothelinAreceptorantagonistsPD156707(CI-1020)andPD180988(CI-1034)reversethehypoxicpulmonary

vasoconstrictionintheperinatallamb.JPharmacolExpTher.2002Aug;3

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