BMS-813160-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-813160Cat.No.:HY-109593CASNo.:1286279-29-5分⼦式:C₂₅H₄₀N₈O₂分⼦量:484.64作⽤靶点:CCR作⽤通路:GPCR/GProtein;Immunology/Inflammation储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:25mg/mL(51.58mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0634mL10.3169mL20.6339mL5mM0.4127mL2.0634mL4.1268mL10mM0.2063mL1.0317mL2.0634mL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(protectfromlight)。-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%salineSolubility:≥2.08mg/mL(4.29mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.29mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.29mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BMS-813160有效的、选择性的CCR2/5的双拮抗剂。BMS-813160与CCR2和CCR5结合，IC50分别为6.2和3.6nM。BMS-813160可⽤于炎症的研究。IC50&TargetCCR5CCR23.6nM(IC50)6.2nM(IC50)体外研究BMS-813160bindswithCCR2,CCR5,CCR1,CCR4andCXCR2withIC50sof6.2nM,3.6nM,＞25μM,＞40μMand＞40μM,respectively[2].BMS-813160showsactivitiestoCCR2CTX,CCR2CD11b,CCR5CTXandCCR5CD11bwithIC50sof0.8,4.8,1.1and5.7nM,respectively[2].体内研究BMS-813160(10-160mg/kg;p.o.twiceadayfortwodays)inhibitsthemigrationofinflammatorymonocytesandmacrophagesinmousethioglycollate-inducedperitonitismodel,andshowsexcellentoralbioavailability[2].AnimalModel:Human-CCR2knock-inC57BL/6malemicewiththioglycollateinjection[2]Dosage:10,50and160mg/kgAdministration:Oralgavage;10-160mg/kgtwiceaday;fortwodaysResult:Dose-dependentlyreducedinflammatorymonocyteandmacrophageinfiltrationintheperitoneum.户使⽤本产品发表的科研⽂献•ResearchSquarePreprint.2020Oct.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CherneyRJ,etal.BMS-813160:APotentCCR2andCCR5DualAntagonistSelectedasaClinicalCandidate.ACSMedChemLett.2021Oct15;12(11):1753-1758.[2].NormanP.etal.AdualCCR2/CCR5chemokineantagonist,BMS-813160?EvaluationofWO2011046916.ExpertOpinTherPat.2011Dec;21(12):1919-24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication