Bay-59-3074-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBay59-3074Cat.No.:HY-100488CASNo.:406205-74-1分⼦式:C₁₈H₁₃F₆NO₄S分⼦量:453.36作⽤靶点:CannabinoidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥34mg/mL(75.00mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2058mL11.0288mL22.0575mL5mM0.4412mL2.2058mL4.4115mL10mM0.2206mL1.1029mL2.2058mL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.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.51mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Bay59-3074⼀种选择性的CB1/CB2受体的部分激动剂，其在CB1和CB2受体中的Ki值分别为48.3nM和45.5nM。Bay59-3074可⽤于缓解疼痛的研究。IC50&TargetCB1CB248.3nM(Ki)45.5nM(Ki)体内研究BAY59-3074(0.3-3mg/kg;oraladministration;daily;for2weeks;maleWistarrats)treatmentimprovesantihyperalgesicandantiallodyniceffectsagainstthermalormechanicalstimuliinratmodelsofchronicneuropathicandinflammatorypain.AnimalModel:MaleWistarrats(160-250g)[1]Dosage:0.3mg/kg,1mg/kg,and3mg/kgAdministration:Oraladministration;daily;for2weeks.Result:Antiallodynicefficacyinthesparednerveinjurymodelwasmaintainedafter2weeksofdailyadministration.Tolerancedevelopedrapidly(within5days)forcannabinoid-relatedsideeffects.Antihyperalgesicandantiallodynicefficacywasmaintained/increased.REFERENCES[1].DeVryJetal.3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate(BAY59-3074):anovelcannabinoidCb1/Cb2receptorpartialagonistwithantihyperalgesicandantiallodyniceffects.JPharmacolExpTher.2004Aug;310(2):620-32McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T