GR-46611-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGR-46611Cat.No.:HY-101248CASNo.:185259-85-2分⼦式:C₂₃H₂₇N₃O₂分⼦量:377.48作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(264.91mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6491mL13.2457mL26.4915mL5mM0.5298mL2.6491mL5.2983mL10mM0.2649mL1.3246mL2.6491mL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(protectfromlight)。-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。BIOLOGICALACTIVITY⽣物活性GR-46611⼀种5-HT1D受体激动剂。GR-46611可⽤于膀胱多动症、⽩⾎病的研究。IC50&Target5-HT1DReceptor体外研究GR-46611(1μM,48h)inducesCEMcellproliferation[2].CellProliferationAssay[2]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:CEMcells(humanTlymphoblasticleukemiacellline)Concentration:1μMIncubationTime:48hResult:Inducedasignificantincreaseincellproliferationby37.0%.体内研究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