Nidufexor-LMB763-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENidufexorCat.No.:HY-109096CASNo.:1773489-72-7Synonyms:LMB763分?式:C??H??ClN?O?分?量:487.93作?靶點:FXR;Autophagy作?通路:MetabolicEnzyme/Protease;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:83.33mg/mL(170.78mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0495mL10.2474mL20.4947mL5mM0.4099mL2.0495mL4.0989mL10mM0.2049mL1.0247mL2.0495mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.26mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.26mM);ClearsolutionBIOLOGICALACTIVITY?物活性Nidufexor(LMB763)?種?服有效的法尼醇X受體(FXR)激動劑，可?于?精性脂性肝炎(NASH)研究[1]。IC50&TargetFXR[1]體內(nèi)研究Nidufexor(LMB763)isapotentandspecificFXR-genemodulatorinvivo,reducingsteatosis,inflammationandfibrosisinnonalcoholicsteatohepatitis(NASH)murinemodels[1].NidufexorexhibitsmoderateCmax(4.5,12.4,28.1,80.9,and140.8μM)andterminaleliminationhalf-lives(t1/2;5.66.3h)followingoraladministration(3,10,30,100,and300mg/kg)inadultmaleWistarHanrats(ageapproximately10weeks)[1]Nidufexorexhibitsterminaleliminationhalf-lives(mouse4.5,rat4.4and,dog6.8h)followingintravenousadministration(mouse3.0,rat5.0and,dog0.5mg/kg)[1].Nidufexorexhibitsterminaleliminationhalf-lives(mouse3.5,rat2.7and,dog10.1h)followingoraladministration(mouse10,rat10and,dog2mg/kg)[1].AnimalModel:Han-Wistarrats[1]Dosage:0.1,0.3,1.5,7.5,25,100mg/kg(PharmacokineticAnalysis)Administration:Oralgavage,oncedailyfor14daysResult:Onday1and13,serumexposureincreasedapproximatelydose-proportionallyfrom0.1to100mg/kg.Exposureat0.1and0.3mg/kgwaslikelyunderestimatedonday13.Nosignificantaccumulationwasobserved[1].REFERENCES[1].ChianelliD,etal.Nidufexor(LMB763),aNovelFXRModulatorfortheTreatmentofNonalcoholicSteatohepatitis.JMedChem.2020Apr23;63(8):3868-3880.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo