JNJ-632-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJNJ-632Cat.No.:HY-112564CASNo.:1572510-42-9分?式:C??H??FN?O?S分?量:378.42作?靶點:HBV作?通路:Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據體外實驗DMSO:125mg/mL(330.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6426mL13.2128mL26.4257mL5mM0.5285mL2.6426mL5.2851mL10mM0.2643mL1.3213mL2.6426mL請根據產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，避免反復凍融造成的產品失效。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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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(5.50mM);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(5.50mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.50mM);ClearsolutionBIOLOGICALACTIVITY?物活性JNJ-632?種?型肝炎病毒(HBV)?組裝調節(jié)劑(CAM)。IC50&TargetHBV[1]體外研究JNJ-632isacapsidassemblymodulatorinhibitinghepatitisBvirus(HBV).JNJ-632inhibitsHBVDNAHepG2.2.15andHBVDNAHepG2.117withEC50sof0.12and0.43μM,respectively.Inthehigh-contentmultiparametercytotoxicity(HepG2),JNJ-632showsEC20sinthe10-30μMrange(consideredweaklycytotoxic)[1].體內研究ThesingledosePKprofileofJNJ-632isevaluatedinC57BL/6micefollowingintravenous(iv)andoral(po)administration.JNJ-632hasamoderateplasmaclearanceof34mL/min/kgandamoderatevolumeofdistributionof1.3L/kg.Theoralbioavailabilityis40%followingoraladministrationof10mg/kgand66%followingoraladministrationof50mg/kg.JNJ-632hasmoderateterminaleliminationhalf-lifewitht1/2sof0.42±0.06h,1.1±0.67h,2.4±2.3h,and5.3±0.1hfor2.5mg/kg(iv),10mg/kg(po),50mg/kg(po),and50mg/kg(sc).Tocircumventthefirstpassmetabolism,JNJ-632isalsodosedsubcutaneouslyat50mg/kginC57BL/6miceandthisresultsinaconcentrationinplasmaafter24hofdosingof102ng/mLandconcentrationinliverafter24hofdosingof1297ng/g[1].PROTOCOLAnimalMice[1]Administration[1]ThepharmacokineticprofileisevaluatedinfedmaleC57BL/6mice(n=3/group).Micearei.v.injectedwithJNJ-632at2.5mg/kg,formulatedasa0.5mg/mLsolutioninPEG400/water(70/30),andbloodsamplesarecollectedfromthesaphenousveinat0.05,0.17,0.5,1,2,4,7,and24hoursintoEDTA-containingmicrocentrifugetubes.JNJ-632isadministeredp.o.at10and50mg/kg,formulatedas0.5and2.5mg/mLsuspensioninmethocel0.5%w/v,andbloodsamplesarecollectedfromthesaphenousveinat0.5,1,2,4,7,9and24hoursintoEDTA-containingmicrocentrifugetubes.JNJ-632isadministereds.c.at50mg/kg,andbloodsamplesarecollected.Thebloodsamplesareimmediatelycentrifugedat4°Candtheplasmawasstoredat-20°C[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].VandyckK,etal.SynthesisandEvaluationofN-Phenyl-3-sulfamoyl-benzamideDerivativesasCapsidAssemblyModulatorsInhibitingHepatitisBVirus(HBV).JMedChem.2018Jul26;61(14):6247-6260.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnot