BMS-779788-EXEL04286652-DataSheet-生命科學(xué)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(diǎn):LXR作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(196.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9644mL9.8220mL19.6440mL5mM0.3929mL1.9644mL3.9288mL10mM0.1964mL0.9822mL1.9644mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)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(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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%saline1/3MasterofBioactiveMolecules—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(dòng)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(nèi)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(chǎn)品發(fā)表的科研?獻(xiàn)?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