Bay-59-3074-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBay59-3074Cat.No.:HY-100488CASNo.:406205-74-1分?式:C??H??F?NO?S分?量:453.36作?靶點(diǎn):CannabinoidReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥34mg/mL(75.00mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2058mL11.0288mL22.0575mL5mM0.4412mL2.2058mL4.4115mL10mM0.2206mL1.1029mL2.2058mL請(qǐng)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(qǐng)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。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.51mM);ClearsolutionBIOLOGICALACTIVITY?物活性Bay59-3074?種選擇性的CB1/CB2受體的部分激動(dòng)劑，其在CB1和CB2受體中的Ki值分別為48.3nM和45.5nM。Bay59-3074可?于緩解疼痛的研究。IC50&TargetCB1CB248.3nM(Ki)45.5nM(Ki)體內(nèi)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