GR79236-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGR79236Cat.No.:HY-18978CASNo.:124555-18-6分⼦式:C₁₅H₂₁N₅O₅分⼦量:351.36作⽤靶点:AdenosineReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:100mg/mL(284.61mM;Needultrasonic)DMSO:≥100mg/mL(284.61mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8461mL14.2304mL28.4608mL5mM0.5692mL2.8461mL5.6922mL10mM0.2846mL1.4230mL2.8461mL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(7.12mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.12mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.12mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GR79236⼀种⾼效，选择性和具有⼝服活性的腺苷A1受体(adenosineA1receptor)激动剂，对于A1和A2受体的Ki值分别为3.1nM和1300nM。GR79236具有抗伤害和抗炎作⽤。IC50&TargetKi:3.1nM(AdenosineA1receptor)and1300nM(AdenosineA2receptor)[1]体外研究GR79236inhibitsIsoprenaline-stimulatedcAMPaccumulationinDDT-MF2cellswithanIC50of2.6nM[1].GR79236inhibitscatecholamine-inducedlipolysisinhuman,ratanddogisolatedadipocytes[3].体内研究GR79236decreaseslocomotoractivityandinhibitsDMCM-inducedseizuresinmice(ED50sof0.13mg/kgand0.3mg/kg,respectively)[1].OraladministrationofGR79236(0.1-10mg/kg)tofedratsinducesminimalchangesintheplasmaconcentrationofnon-esterifiedfattyacidsandinthebloodconcentrationsofglucoseandlactate[3].IntravenousinfusionofGR79236tofastedpithedrats,ororaladministrationofGR79236tofastedconsciousratsanddogs,producestime-anddose-dependentdecreasesintheplasmanon-esterifiedfattyacidconcentration.Inthefastedrats,dosesofGR79236thatloweredplasmalevelsofnon-esterifiedfattyacidsalsoproducedhypotriglyceridaemiaandanti-ketoticeffects[3].REFERENCES[1].SneydJR,etal.MulticentreevaluationoftheadenosineagonistGR79236Xinpatientswithdentalpainafterthirdmolarextraction.BrJAnaesth.2007May;98(5):672-676.[2].LJKnutsen,etal.N-substitutedadenosinesasnovelneuroprotectiveA(1)agonistswithdiminishedhypotensiveeffects.JMedChem.1999Sep9;42(18):3463-77.[3].PStrong,etal.Suppressionofnon-esterifiedfattyacidsandtriacylglycerolinexperimentalanimalsbytheadenosineanalogueGR79236.ClinSci(Lond).1993Jun;84(6):663-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed