BMS-813160-DataSheet-生命科學(xué)試劑-MedChemExpressVIP

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBMS-813160Cat.No.:HY-109593CASNo.:1286279-29-5分?式:C??H??N?O?分?量:484.64作?靶點(diǎn):CCR作?通路:GPCR/GProtein;Immunology/Inflammation儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(51.58mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0634mL10.3169mL20.6339mL5mM0.4127mL2.0634mL4.1268mL10mM0.2063mL1.0317mL2.0634mL請(qǐng)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(qǐng)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(protectfromlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.29mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.29mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.29mM);ClearsolutionBIOLOGICALACTIVITY?物活性BMS-813160有效的、選擇性的CCR2/5的雙拮抗劑。BMS-813160與CCR2和CCR5結(jié)合，IC50分別為6.2和3.6nM。BMS-813160可?于炎癥的研究。IC50&TargetCCR5CCR23.6nM(IC50)6.2nM(IC50)體外研究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].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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