Rimonabant-Hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemERimonabantHydrochlorideCat.No.:HY-14137CASNo.:158681-13-1分⼦式:C₂₂H₂₂Cl₄N₄O分⼦量:500.25作⽤靶点:CannabinoidReceptor;Bacterial作⽤通路:GPCR/GProtein;NeuronalSignaling;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(66.63mM;Needultrasonic)扫描⼆维码，运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9990mL9.9950mL19.9900mL5mM0.3998mL1.9990mL3.9980mL10mM0.1999mL0.9995mL1.9990mL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，并请注意储备液的保存⽅式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:2.5mg/mL(5.00mM);Suspendedsolution;Needultrasonic此⽅案可获得2.5mg/mL(5.00mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。1/3www.MedChemEwww.MedChemE2.请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.5mg/mL(5.00mM);Clearsolution此⽅案可获得≥2.5mg/mL(5.00mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性RimonabanthHydrochloride(SR141716AHydrochloride)中⼼⼤⿇素受体1(CB1)⾼效的、选择性的反向激动剂，Ki值为1.8nM。RimonabanthHydrochloride(SR141716AHydrochloride)也能够抑制分枝杆膜蛋⽩3(MMPL3)。IC50&TargetCB11.8nM(Ki)体外研究RimonabantcouldinhibitthegrowthofMtbwithanMICof54μM.MmpL3,ananti-TBtarget,isthedirecttargetofrimonabant[2].Rimonabantitself(10-12-10-3M,12concentrations)inhibitsthebasalbindingof[35S]GTPgStohumancorticalmembranesinaconcentrationdependentmanner,witha-logIC50of4.7±0.2(IC50=20μM)andamaximalinhibitionof48±2%[3].体内研究Rimonabant(10mg/kgbygavage)isfedfor2weeksto3-month-oldmaleobeseZuckerratsasanimpairedglucosetolerancemodelandfor10weeksto6-month-oldmaleobeseZuckerratsasamodelofthemetabolicsyndrome.RANTESandMCP-1serumlevelsareincreasedinobesevsleanZuckerratsandsignificantlyreducedbylong-termtreatmentwithRimonabant,whichslowesweightgaininratswiththemetabolicsyndrome.NeutrophilsandmonocytesaresignificantlyincreasedinyoungandoldobesevsleanZuckerratsandloweredbyRimonabant.Platelet-boundfibrinogenissignificantlyenhancedinobesevsleanZuckerratsofbothage,andisreducedbyRimonabant[1].Rimonabant(20mgdaily)exhibitsasignificantreductioninmanycardiometabolicriskfactors[4].户使⽤本产品发表的科研⽂献•Cell.2019Jan24;176(3):636-648.e13.•Autophagy.2021Feb25;1-15.•Cancers(Basel).2021Jan18;13(2):330.•Neuroscience.2019Feb19.pii:S0306-4522(19)30117-4.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SeelyKA,etal.AM-251andrimonabantactasdirectantagonistsatmu-opioidreceptors:Implicationsforopioid/cannabinoidinteractionstudies.Neuropharmacology.2012Oct;63(5):905-15.2/3www.MedChemEwww.MedChemE[2].ZhangB,etal.CrystalStructuresofMembraneTransporterMmpL3,anAnti-TBDrugTarget.Cell.2019Jan24;176(3):636-648.e13.[3].Erdozain,A.M.etal.TheinverseagonisteffectofrimonabantonGproteinactivationisnotmediatedbythecannabinoidCB1receptor:EvidencefrompostmortemhumanbrainBiochemicalPharmacology(2012),83(2),260-268.[4].Erdozain,A.M.etal.TheinverseagonisteffectofrimonabantonGproteinactivationisnotmediatedbythecannabinoidCB1receptor:EvidencefrompostmortemhumanbrainBiochemicalPharmacology(2012),83(2),260-268.McePdfHeight关注MCE中国公众号，

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