JD-5037-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJD-5037Cat.No.:HY-18697CASNo.:1392116-14-1分?式:C??H??Cl?N?O?S分?量:572.51作?靶點:CannabinoidReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(436.67mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7467mL8.7335mL17.4669mL5mM0.3493mL1.7467mL3.4934mL10mM0.1747mL0.8733mL1.7467mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.75mg/mL(4.80mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(4.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性JD-5037CB1R有效拮抗劑，IC50值為1.5nM。IC50&TargetCB11.5nM(IC50)體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedform