URB937-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEURB937Cat.No.:HY-116477CASNo.:1357160-72-5分?式:C??H??N?O?分?量:354.4作?靶點:FAAH作?通路:MetabolicEnzyme/Protease;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(705.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8217mL14.1084mL28.2167mL5mM0.5643mL2.8217mL5.6433mL10mM0.2822mL1.4108mL2.8217mL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。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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:≥2.08mg/mL(5.87mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.87mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.87mM);ClearsolutionBIOLOGICALACTIVITY?物活性URB937?服有效的、外周限制的FAAH抑制劑，IC50值為26.8nM，可增加anandamide?平。URB937不能響腦內(nèi)FAAH?平(?法透過?腦屏障)。IC50&TargetIC50:26.8nM(FAAH)[1].體外研究URB937isactivelyextrudedfromtheCNSbytheATP-bindingcassette(ABC)membranetransporter,Abcg2[3].體內(nèi)研究URB937(1mg/kg,i.p.)administratedinmiceincreasesanandamidelevelsinperipheraltissues,butnotforebrainorhypothalamus[1].URB937(1mg/kg,s.c.)suppressespainresponseselicitedbyi.p.injectionsofaceticacid[1].URB937inmalerats(anoraldose3mg/kg,F=36%)isabsorbedatamoderaterateanddisplaysapeakplasmaconcentration(Cmax)of159.47ng/ml,whichwasachievedonehourafteradministration.URB937exhibitsT1/2of60minbyanoraldoseof3mg/kg[2].URB937producesahighdegreeofantinociceptioninfemalemiceandratsinmodelsofvisceralandinflammatorypain.Moreover,thecompounddisplayedarestrictedaccesstoplacentalandfetaltissuesinpregnantmiceandrats[3].URB937(1mg/kg,every2daysfor30days)attenuatesradiation-inducedlunginjuryandincreasedendocannabinoidconcentrationinlungtissue[4].AnimalModel:SwissWebstermice[1].Dosage:1mg/kg.Administration:S.C.Result:Suppressesdpainresponseselicitedbyi.p.injectionsofaceticacid.AnimalModel:AdultSpragueDawleymaleandfemalerats(250-300g)[2].Dosage:0.3,1,3,10mg/kg(PharmacokineticAnalysis).Administration:Singleoraldose.Result:InhibitedliverFAAHactivitywithamedianeffectivedose(ED50)of0.9mg/kg.InhibitsFAAHinperipheraltissuesandidentifyapossiblebiomarkerfortargetengagement.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].JasonRClapper,etal.Anandamidesuppressespaininitiationthroughaperipheralendocannabinoidmechanism.NatNeurosci.2010Oct;13(10):1265-70.[2].ValentinaVozella,etal.Pharmacokinetics,pharmacodynamicsandsafetystudiesonURB937,aperipherallyrestrictedfattyacidamidehydrolase(FAAH)inhibitor,inrats.JPharmPharmacol.2019Dec;71(12):1762-1773.[3].GMoreno-Sanz,etal.PharmacologicalcharacterizationoftheperipheralFAAHinhibitorURB937infemalerodents:interactionwiththeAbcg2transporterintheblood-placentabarrier.BrJPharmacol.2012Dec;167(8):1620-8.[4].RuiLi,etal.TheFattyAcidAmideHydrolaseInhibitorURB937AmelioratesRadiation-InducedLungInjuryinaMouseModel.Inflammation.2017Aug;40(4):1254-1263.McePdfHeightCaution:Product