Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGR-46611Cat.No.:HY-101248CASNo.:185259-85-2分?式:C??H??N?O?分?量:377.48作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?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:100mg/mL(264.91mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6491mL13.2457mL26.4915mL5mM0.5298mL2.6491mL5.2983mL10mM0.2649mL1.3246mL2.6491mL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(protectfromlight)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。BIOLOGICALACTIVITY?物活性GR-46611?種5-HT1D受體激動劑。GR-46611可?于膀胱多動癥、??病的研究。IC50&Target5-HT1DReceptor體外研究GR-46611(1μM,48h)inducesCEMcellproliferation[2].CellProliferationAssay[2]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:CEMcells(humanTlymphoblasticleukemiacellline)Concentration:1μMIncubationTime:48hResult:Inducedasignificantincreaseincellproliferationby37.0%.體內(nèi)研究GR-46611(1mg/kg,i.p.)significantlyimprovessurvivalofDravetsyndrome(DS)mice[1].GR-46611(0.03-300μg/kg,i.v.)increasesthresholdvolume,bladdercapacity,andresidualvolumeinchronicspinalcordinjury(SCI)cats[3].GR46611(3-30mg/kg,s.c.)causesadose-relateddecreaseinrectaltemperatureintheadultguinea-pig[4].AnimalModel:Dravetsyndrome(DS)mice[1]Dosage:0.01,0.1and1mg/kgAdministration:Intraperitonealinjection(i.p.)Result:Improvedsurvivalrelativetovehicletreatedcontrolswith89%survivingrate.REFERENCES[1].PaulGHatini,etal.A5-HT1D-receptoragonistprotectsDravetsyndromemicefromseizureandearlydeath.EurJNeurosci.2020Nov;52(10):4370-4374.[2].CSibella-Argüelle,etal.TheproliferationofhumanTlymphoblasticcellsinducedby5-HT1Breceptorsactivationisregulatedby5-HT-moduline.CRAcadSciIII.2001Apr;324(4):365-72.[3].BaojunGu,etal.Inhibitionofbladderactivityby5-hydroxytryptamine1serotoninreceptoragonistsincatswithchronicspinalcordinjury.JPharmacolExpTher.2004Sep;310(3):1266-72.[4].MSkingle,etal.Stimulationofcentral5-HT1Dreceptorscauseshypothermiaintheguinea-pig.JPsychopharmacol.1994Jan;8(1):14-21.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea