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MK-5596

Cat.No.:HY-10575

CASNo.:1044586-68-6

分⼦式:C₂₇H₂₃Cl₃N₄O₂

分⼦量:541.86

作⽤靶点:CannabinoidReceptor;CytochromeP450

作⽤通路:GPCR/GProtein;NeuronalSignaling;Metabolic

Enzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性MK-5596是⼀种⾼效、选择性好、⼝服有效的CB1R(IC50=1.0nM,EC50=5.8nM)反向激动剂。MK-5596

对hERG抑制活性弱。MK-5596具有强效的减重和抑制⾷欲作⽤。MK-5596对CYP酶(CYP3A4：IC50=3.3

μM，CYP2C8：IC50=11μM，CYP2C9：IC50=18μM，CYP2D6：IC50=6μM)有⼀定抑制作⽤。MK-

5596可以⽤于肥胖等疾病的研究[1]。

IC50TargetCB1CYP3A4CB1CYP2C8

1.0nM(IC50)3.3μM(IC50)5.8nM(EC50)11μM(IC50)

CYP2C9CYP2D6

18μM(IC50)6μM(IC50)

REFERENCES

[1].YanL,etal.DiscoveryofN-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[