Olorinab-APD-371-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOlorinabCat.No.:HY-111110CASNo.:1268881-20-4Synonyms:APD371分?式:C??H??N?O?分?量:357.41作?靶點:CannabinoidReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(559.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7979mL13.9895mL27.9791mL5mM0.5596mL2.7979mL5.5958mL10mM0.2798mL1.3990mL2.7979mL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(sealedstorage,awayfrommoisture)。-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:≥5mg/mL(13.99mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥5mg/mL(13.99mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(13.99mM);ClearsolutionBIOLOGICALACTIVITY?物活性O(shè)lorinab(APD371)??素受體2型(CB2)強有效的、選擇性的全激動劑，其對hCB2的EC50值為6.2nM。IC50&TargetEC50:6.2nM(hCB2)[1].體外研究AcomprehensiveinvitroprofileofOlorinab(APD371)(6)showsthatsingledigitnanomolarpotencyandfullintrinsicefficacyaremaintainedinallspeciesassessed,andthatOlorinab(APD371)ishighlyselectiveforCB2overCB1inbothbindingandfunctionalassays.Furthermore,Olorinab(APD371)inducesefficientreceptorinternalization(~106%relativetotheCB1/2agonistCP55,940)inCHOcellsexpressingHA-taggedratCB2suggestingthat,accordingtothehypothesis,Olorinab(APD371)wouldbeabletodriveagonist-inducedreceptorrecycling[1].體內(nèi)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