Rimonabant-Hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemERimonabantHydrochlorideCat.No.:HY-14137CASNo.:158681-13-1分?式:C??H??Cl?N?O分?量:500.25作?靶點:CannabinoidReceptor;Bacterial作?通路:GPCR/GProtein;NeuronalSignaling;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:33.33mg/mL(66.63mM;Needultrasonic)掃描?維碼，運?溶解?案計算器獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9990mL9.9950mL19.9900mL5mM0.3998mL1.9990mL3.9980mL10mM0.1999mL0.9995mL1.9990mL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備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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%DMSO40%PEG3005%Tween-8045%salineSolubility:2.5mg/mL(5.00mM);Suspendedsolution;Needultrasonic此?案可獲得2.5mg/mL(5.00mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(5.00mM);Clearsolution此?案可獲得≥2.5mg/mL(5.00mM，飽和度未知)的澄溶液，此?案不適?于實驗周期在半個?以上的實驗。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性RimonabanthHydrochloride(SR141716AHydrochloride)中???素受體1(CB1)?效的、選擇性的反向激動劑，Ki值為1.8nM。RimonabanthHydrochloride(SR141716AHydrochloride)也能夠抑制分枝桿膜蛋?3(MMPL3)。IC50&TargetCB11.8nM(Ki)體外研究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].體內(nèi)研究Rimonabant(10mg/kgbygavage)isfedfor2weeksto3-month-oldmaleobeseZuckerratsasanimpairedglucosetolerancemodelandfor10weeksto6-month-oldmaleobeseZuckerratsasamodelofthemetabolicsyndrome.RANTESandMCP-1serumlevelsareincreasedinobesevsleanZuckerratsandsignificantlyreducedbylong-termtreatmentwithRimonabant,whichslowesweightgaininratswiththemetabolicsyndrome.NeutrophilsandmonocytesaresignificantlyincreasedinyoungandoldobesevsleanZuckerratsandloweredbyRimonabant.Platelet-boundfibrinogenissignificantlyenhancedinobesevsleanZuckerratsofbothage,andisreducedbyRimonabant[1].Rimonabant(20mgdaily)exhibitsasignificantreductioninmanycardiometabolicriskfactors[4].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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關(guān)注MCE中國公眾號，

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