BMS-779788-EXEL04286652-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBMS-779788Cat.No.:HY-19919CASNo.:918348-67-1Synonyms:EXEL04286652;XL-652;BMS-788分?式:C??H??ClN?O?S分?量:509.06作?靶點:LXR作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:100mg/mL(196.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9644mL9.8220mL19.6440mL5mM0.3929mL1.9644mL3.9288mL10mM0.1964mL0.9822mL1.9644mL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?式選擇適當的溶解?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?現配，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沉淀、析出現象，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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(4.91mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.91mM);ClearsolutionBIOLOGICALACTIVITY?物活性BMS-779788LXR的部分激動劑，其對LXRα和LXRβ的IC50值分別為68和14μM。IC50&TargetIC50:68nM(LXRα);14nM(LXRβ)[1]體外研究TheLXRselectivepartialagonistBMS-779788isidentifiedwithpotentinductionofATPbindingtransportersABCA1andABCG1inhumanwholeblood(EC50=1.2μM,55%efficacy)[2].體內研究BMS-779788inducesLXRtargetgenesinbloodinvivowithanEC50=610nM,avaluesimilartoitsinvitrobloodgeneinductionpotency.BMS-779788is29-and12-foldlesspotentthanthefullagonistT0901317inelevatingplasmatriglycerideandLDLcholesterol,respectively,withsimilarresultsforplasmacholesterylestertransferproteinandapolipoproteinB[1].InmiceBMS-779788displaysperipheralinductionofABCA1at3and10mpkdoseswithnosignificantelevationofplasmaorhepatictriglyceridesatthesedoses,showinganimprovedprofilecomparedtoafullpan-agonist[2].PROTOCOLAnimalMonkeys:Malecynomolgusmonkeysareusedinthestudy.Forasingle-dosepharmacokinetic(PK)-Administration[1]pharmacodynamic(PD)study,2animalseacharetreatedeitherwithvehicle[0.5%carboxymethylcelluloseand2%Tween80inpurifiedwater)or1mg/kgBMS-779788.Forthe7dayPDstudy,18animalsarerandomizedinto6treatmentgroups(N=3/group;3-6kg)andreceivedthefollowingtreatmentsat7AMdailyfor7daysbyoralgavage:vehicle,10mg/kgperdayT0901317and0.3,1,3,or10mg/kgperdayBMS-779788[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?RadboudUniversityNijmegen.2021Mar.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KirchgessnerTG,etal.PharmacologicalcharacterizationofanovelliverXreceptoragonistwithpartialLXRαactivityandafavorablewindowinnonhumanprimates.JPharmacolExpTher.2015Feb;352(2):305-14.[2].KickE,etal.LiverXreceptor(LXR)partialagonists:biarylpyrazolesandimidazolesdisplayingapreferenceforLXRβ.BioorgMedChemLett.2015Jan15;25(2):372-7.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyv