JD-5037-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJD-5037Cat.No.:HY-18697CASNo.:1392116-14-1分⼦式:C₂₇H₂₇Cl₂N₅O₃S分⼦量:572.51作⽤靶点:CannabinoidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(436.67mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7467mL8.7335mL17.4669mL5mM0.3493mL1.7467mL3.4934mL10mM0.1747mL0.8733mL1.7467mL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。-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:≥2.75mg/mL(4.80mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(4.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JD-5037CB1R有效拮抗剂，IC50值为1.5nM。IC50&TargetCB11.5nM(IC50)体内研究JD5037(3mg/kg/d,i.p.)inducesequalreductionsinbodyweight,attenuatestheHFD-inducedhyperglycemia,andreducestheHFD-inducedhepaticinjuryandsteatosisinobeseMagel2-nullmice[2].JD5037(3mg/kg/day,p.o.)significantlyreducesthesizeoftumorsandabrogatesthetumorinDEN-treatedmice.JD5037attenuatestheAEAlevelsinHCCsamplesfrommice[3].PROTOCOLAnimalMice:JD-5037isformulatedinvehicle(V;1%Tween80,4%DMSO,95%Saline).ObesemicearetreatedAdministration[2]chronically(28d)withvehicle(V;1%Tween80,4%DMSO,95%Saline),JD5037,orSLV319atadoseof3mg/kg,i.p.Bodyweightandfoodintakearemonitoreddaily.Miceareeuthanizedbycervicaldislocationunderanesthesia;thebrain,hypothalamus,liver,andcombinedfatpadsareremoved,weighed,andsnap-frozen,andtrunkbloodiscollectedfordeterminingtheendocrineandbiochemicalparameters[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2022Apr4;13(1):1783.•JAmSocNephrol.2017Dec;28(12):3518-3532.•BrJPharmacol.2020Jan;177(1):110-127.•Diabetes.2020Oct;69(10):2120-2132.•Elife.2020Nov19;9:e60771.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChorvatRJ.PeripherallyrestrictedCB1receptorblockers.BioorgMedChemLett.2013Sep1;23(17):4751-60.[2].KnaniI,etal.Targetingtheendocannabinoid/CB1receptorsystemfortreatingobesityinPrader-Willisyndrome.MolMetab.2016Oct22;5(12):1187-1199.[3].MukhopadhyayB,etal.Cannabinoidreceptor1promoteshepatocellularcarcinomainitiationandprogressionthroughmultiplemechanisms.Hepatology.2015May;61(5):1615-26.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedform