Phensuximide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEPhensuximideCat.No.:HY-B1730CASNo.:86-34-0分⼦式:C₁₁H₁₁NO₂分⼦量:189.21作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(1321.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.2851mL26.4257mL52.8513mL5mM1.0570mL5.2851mL10.5703mL10mM0.5285mL2.6426mL5.2851mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Phensuximide⼀种琥珀酰亚胺类抗癫痫(antiepileptic)和抗惊厥(anticonvulsant)试剂。Phensuximide可以抑制去极化脑组织中cyclicAMP和cyclicGMP的积累。在动物模型中，Phensuximide可⽤于癫痫研究的相关研究。IC50&TargetIC50:cyclicAMPandcyclicGMPaccumulation[2]体外研究Phensuximideproducedepolarization-inducedaccumulationofcyclicGMPorcyclicAMPlevelswithID501/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEvaluesof8.00mMor6.20mMinincubatedslicesofmousecerebralcortex[2].Phensuximide(0.5-2.0mM)hastheabilitytocompetitivelyinhibitmephenytoin4-hydroxylaseactivityinhumanlivermicrosomes,theKiandKmvaluesare559μMand235μM,respectively[4].体内研究Phensuximide(intraperitonealinjection;1.25mmol/kg;singledose)inducesmildchangesinrenalfunction,including:tracehematuria,increasedproteinuriaanddecreasedpaminohippurateuptakeinSprague-Dawleyrats[1].Phensuximide(intraperitonealinjection;0.3or0.6mmol/kg;5-7days)resultsintransienthematuriaandproteinuria,butnochangeintheotherrenalfunctionparametersstudied.Itisconcludedthatphensuximideproducesmild,transientrenaleffectsinFischer344rats,andthattheFischer344ratisasuitablemodelforstudyingphensuximide-inducedtoxicitytotheurinarytract[1].AnimalModel:Fischer344rats[1]Dosage:0.3or0.6mmol/kgAdministration:Intraperitonealinjection;5-7daysResult:Inducedurotoxicityfollowingdailyadministrationfor5-7daysinFischer344rats.REFERENCES[1].GORankin,etal.UrinaryTractEffectsofPhensuximideintheSprague-DawleyandFischer344Rat.JApplToxicol..1986Oct;6(5):349-56.[2].JAFerrendelli,etal.InhibitoryEffectsofAnticonvulsantDrugsonCyclicNucleotideAccumulationinBrain.AnnNeurol.1979Jun;5(6):533-8.[3].JGMILLICHAP,etal.Milontin:ANewDrugintheTreatmentofPetitMal.Lancet.1952Nov8;2(6741):907-10.[4].SDHall,etal.Characterizationandinhibitionofmephenytoin4-hydroxylaseactivityinhumanlivermicrosomes.TheJOURNALOPPHARMAcOLOGYANDEXPERIMENTALTHERAPEUTICSMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat