Olorinab-APD-371-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOlorinabCat.No.:HY-111110CASNo.:1268881-20-4Synonyms:APD371分⼦式:C₁₈H₂₃N₅O₃分⼦量:357.41作⽤靶点:CannabinoidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:200mg/mL(559.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7979mL13.9895mL27.9791mL5mM0.5596mL2.7979mL5.5958mL10mM0.2798mL1.3990mL2.7979mL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(sealedstorage,awayfrommoisture)。-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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(13.99mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(13.99mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(13.99mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Olorinab(APD371)⼤⿇素受体2型(CB2)强有效的、选择性的全激动剂，其对hCB2的EC50值为6.2nM。IC50&TargetEC50:6.2nM(hCB2)[1].体外研究AcomprehensiveinvitroprofileofOlorinab(APD371)(6)showsthatsingledigitnanomolarpotencyandfullintrinsicefficacyaremaintainedinallspeciesassessed,andthatOlorinab(APD371)ishighlyselectiveforCB2overCB1inbothbindingandfunctionalassays.Furthermore,Olorinab(APD371)inducesefficientreceptorinternalization(~106%relativetotheCB1/2agonistCP55,940)inCHOcellsexpressingHA-taggedratCB2suggestingthat,accordingtothehypothesis,Olorinab(APD371)wouldbeabletodriveagonist-inducedreceptorrecycling[1].体内研究Olorinab(APD371)significantlyincreasespawwithdrawalthresholdsatdoses≥3mg/kgPO(ED50=2.3mg/kg).Inaseparateexperiment,asingledoseofOlorinab(APD371)(10mg/kg,PO)inhibitspawwithdrawalthresholdforupto4hoursafteradministration.Seperately,theanalgesiceffectsofOlorinab(APD371)areshowntobehighlylikelymediatedviaactivityatCB2receptors[1].REFERENCES[1].HanS,etal.DiscoveryofAPD371:IdentificationofaHighlyPotentandSelectiveCB2AgonistfortheTreatmentofChronicPain.ACSMedChemLett.2017Nov30;8(12):1309-1313.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications