MK-3207-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMK-3207Cat.No.:HY-10301CASNo.:957118-49-9分⼦式:C₃₁H₂₉F₂N₅O₃分⼦量:557.59作⽤靶点:CGRPReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:≥150mg/mL(269.01mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7934mL8.9672mL17.9343mL5mM0.3587mL1.7934mL3.5869mL10mM0.1793mL0.8967mL1.7934mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.48mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.48mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.48mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MK-3207⼀种⼝服有效的、具有⾼选择性和种属特异性的CGRP受体拮抗剂(对⼈CGRP受体：IC50=0.12nM;Ki=0.024nM)。MK-3207可⽤于偏头痛的研究。体外研究MK-3207(0.3,0.6,1.1,2.3,4.5,9.0nM;30min)potentlyblockshumanα-CGRP-stimulatedcAMPresponsesinhumanCGRPreceptor-expressingHEK293cells[1].CellViabilityAssay[1]CellLine:HEK293cells(stablyexpressinghumanCLR/RAMP1)Concentration:0.3,0.6,1.1,2.3,4.5,9.0nMIncubationTime:30min(pre-treat)Result:Blockedhumanα-CGRP-stimulatedcAMPresponseswithanIC50valueof0.12nM.体内研究MK-3207(0.3,0.6,2.1,9.1,21.2,60.6µg/kg;i.v.;single)inhibitsCIDVinrhesusmonkeyswithEC50andEmaxvaluesofapproximately0.8nMand81%[1].MK-3207(10mg/kg;p.o.;single)showstheCSF/plasmaratiois2to3%[1].AnimalModel:Adultrhesusmonkeys(4.8-12.7kg;capsaicin-induced)[1].Dosage:0.3,0.6,2.1,9.1,21.2,60.6µg/kgAdministration:Intravenousinjection;single.Result:Resultedinanexposure-dependentdecreaseincapsaicin-induceddermalvasodilationintherhesusmonkeyforearm.AnimalModel:Adultrhesusmonkeys(4.8-12.7kg)[1].Dosage:10mg/kgAdministration:Oraladministration;single.Result:ExhibitedtheCSF/plasmaratiowas2to3%,howevertheCSF/plasmaratiowasapproximately30%oftheunboundfraction(9.4%)inplasma.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•VasculPharmacol.2017Mar;90:36-43.•EurJPharmacol.2018Jun15;829:85-92.•Pharmacology.2019;104(5-6):332-341.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SalvatoreCA,MooreEL,CalamariA,PharmacologicalpropertiesofMK-3207,apotentandorallyactivecalcitoningene-relatedpeptidereceptorantagonist.JPharmacolExpTher.2010Apr;333(1):152-60.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf