Phensuximide-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEPhensuximideCat.No.:HY-B1730CASNo.:86-34-0分?式:C??H??NO?分?量:189.21作?靶點:Others作?通路:Others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(1321.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM5.2851mL26.4257mL52.8513mL5mM1.0570mL5.2851mL10.5703mL10mM0.5285mL2.6426mL5.2851mL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，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Phensuximide?種琥珀酰亞胺類抗癲癇(antiepileptic)和抗驚厥(anticonvulsant)試劑。Phensuximide可以抑制去極化腦組織中cyclicAMP和cyclicGMP的積累。在動物模型中，Phensuximide可?于癲癇研究的相關(guān)研究。IC50&TargetIC50:cyclicAMPandcyclicGMPaccumulation[2]體外研究Phensuximideproducedepolarization-inducedaccumulationofcyclicGMPorcyclicAMPlevelswithID501/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEvaluesof8.00mMor6.20mMinincubatedslicesofmousecerebralcortex[2].Phensuximide(0.5-2.0mM)hastheabilitytocompetitivelyinhibitmephenytoin4-hydroxylaseactivityinhumanlivermicrosomes,theKiandKmvaluesare559μMand235μM,respectively[4].體內(nèi)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