RHC-80267-U-57908-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERHC80267Cat.No.:HY-107416CASNo.:83654-05-1Synonyms:U-57908分⼦式:C₂₀H₃₄N₄O₄分⼦量:394.51作⽤靶点:Acyltransferase;mAChR;COX;Phospholipase作⽤通路:MetabolicEnzyme/Protease;GPCR/GProtein;NeuronalSignaling;Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(63.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5348mL12.6740mL25.3479mL5mM0.5070mL2.5348mL5.0696mL10mM0.2535mL1.2674mL2.5348mL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。-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)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.34mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.34mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.34mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性RHC80267(U-57908)⼀种有效的选择性⼆酰⽢油脂酶(DAGL)抑制剂(对⽝⾎⼩板的IC50为4μM)。RHC80267抑制胆碱酯酶活性，IC50为4μM，从⽽增强了⼄酰胆碱引起的松弛。RHC80267还抑制COX活性和磷脂酰胆碱的⽔解。IC50&TargetIC50:4μM(Caninediacylglycerollipase),4μM(Cholinesterase);COX;Phosphatidylcholine[1][3][4]体外研究ThepotentiationbyRHC80267oftherelaxationtoacetylcholinecouldbecausedbytheinhibitionofcholinesterase:(1)RHC80267doesnotaffecttheresponsestocarbachol,thecarbamylderivativeofacetylcholinewhichonlydiffersfromacetylcholinebyitsresistancetohydrolysisbycholinesterase,and(2)theeffectofRHC80267ismimickedbytheinhibitorofcholinesteraseneostigmine,RHC80267showingnoadditionaleffectinthepresenceofamaximallyeffectiveconcentrationofneostigmine.ThedeterminationoftheeffectofRHC80267onthecholinesteraseactivityofbrainhomogenateconfirmedthatRHC80267inhibitsthisenzymeinthesamerangeofconcentrationsincreasingtherelaxationtoacetylcholine,namelyat1-10μM[2].体内研究RHC80267(40μM)enhancescontractionsinducedbyU46619(athromboxaneA2analog)inhumanandratpulmonaryarteries(hPAsandrPAs,respectively)andbyangiotensinII(ANGII)inrPAsinanendothelium-dependentmanner[3].REFERENCES[1].SutherlandCA,etal.RelativeactivitiesofratanddogplateletphospholipaseA2anddiglyceridelipase.SelectiveinhibitionofdiglyceridelipasebyRHC80267.JBiolChem.1982Dec10;257(23):14006-10.[2].GhisdalP,etal.ThediacylglycerollipaseinhibitorRHC-80267potentiatestherelaxationtoacetylcholineinratmesentericarterybyanti-cholinesteraseaction.EurJPharmacol.2005Jul4;517(1-2):97-102.[3].KarpińskaO,etal.ActivationofCB1receptorsby2-arachidonoylglycerolattenuatesvasoconstrictioninducedbyU46619andangiotensinIIinhumanandratpulmonaryarteries.AmJPhysiolRegulIntegrCompPhysiol.2017Jun1;312(6):R883-R893.[4].OglesbyTD,etal.TheinhibitionofarachidonicacidmetabolisminhumanplateletsbyRHC80267,adiacylglycerollipaseinhibitor.BiochimBiophysActa.1984Apr18;793(2):269-77.McePdfHeightCaution:Producthasnotbee