MK-3207-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMK-3207Cat.No.:HY-10301CASNo.:957118-49-9分?式:C??H??F?N?O?分?量:557.59作?靶點(diǎn):CGRPReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥150mg/mL(269.01mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7934mL8.9672mL17.9343mL5mM0.3587mL1.7934mL3.5869mL10mM0.1793mL0.8967mL1.7934mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.48mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.48mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.48mM);ClearsolutionBIOLOGICALACTIVITY?物活性MK-3207?種?服有效的、具有?選擇性和種屬特異性的CGRP受體拮抗劑(對?CGRP受體：IC50=0.12nM;Ki=0.024nM)。MK-3207可?于偏頭痛的研究。體外研究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.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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