BMS-779788-EXEL04286652-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-779788Cat.No.:HY-19919CASNo.:918348-67-1Synonyms:EXEL04286652;XL-652;BMS-788分⼦式:C₂₈H₂₉ClN₂O₃S分⼦量:509.06作⽤靶点:LXR作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(196.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9644mL9.8220mL19.6440mL5mM0.3929mL1.9644mL3.9288mL10mM0.1964mL0.9822mL1.9644mL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。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(4.91mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.91mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BMS-779788LXR的部分激动剂，其对LXRα和LXRβ的IC50值分别为68和14μM。IC50&TargetIC50:68nM(LXRα);14nM(LXRβ)[1]体外研究TheLXRselectivepartialagonistBMS-779788isidentifiedwithpotentinductionofATPbindingtransportersABCA1andABCG1inhumanwholeblood(EC50=1.2μM,55%efficacy)[2].体内研究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.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyv