TRC051384-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETRC051384Cat.No.:HY-101712CASNo.:867164-40-7分⼦式:C₂₅H₃₁N₅O₄分⼦量:465.54作⽤靶点:HSP作⽤通路:CellCycle/DNADamage;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(214.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1480mL10.7402mL21.4804mL5mM0.4296mL2.1480mL4.2961mL10mM0.2148mL1.0740mL2.1480mL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。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.37mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TRC051384热休克蛋⽩70(HSP70)诱导剂。IC50&TargetHSP70体外研究TRC051384,dosedependentlyinducesHSP70BmRNAbyseveralhundredfoldsinbothHeLaandratprimarymixedneurons.TreatmentwithTRC051384resultsinsignificantdose-dependentincreaseinHSF1transcriptionalactivityandrecoveryofluciferaseactivity.TRC051384resultsin60%inhibitionat6.25μMand90%inhibitionat12.5μMofLPS-inducedTNF-αexpressionindifferentiatedTHP-1cellline[1].体内研究TreatmentwithTRC051384significantlyreducesstrokeassociatedneuronalinjury(87%reductioninareaofpenumbrarecruitedtoinfarct,and25%reductioninbrainedema)anddisabilityinaratmodeloftransientischemicstrokeevenwhenadministered8hourspostonsetofischemia.Significantimprovementinsurvival(50%byday2and67.3%byday7)isobservedwithTRC051384treatmentinitiatedat4hoursafterischemiaonset.InductionofHSP70byTRC051384involvesHSF1activationandresultsinelevatedchaperoneandanti-inflammatoryactivity[1].PROTOCOLCellAssay[1]HeLacelltransientlyco-transfectedwithheatshockelements-luciferasereporterandnormalizationvector,β-galactosidasearetreatedwithvehicleorTRC051384(12.5and25μM)for4hours.Celllysatesarethenpreparedandanalyzedforluciferaseandβ-galactosidaseactivity[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:InjuredhemispheresfromvehicletreatedanimalsandTRC051384treatedanimalsarecollectedat10-Administration[1]hourpost-initiationoftMCAo.TotalRNAfromeachbrainsampleisextractedfollowedbycDNApreparation.EachsampleofcDNAisanalyzed[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•DomestAnimEndocrin.2021Jan;74:106533.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].MohananA,etal.DelayedinterventioninexperimentalstrokewithTRC051384--asmallmoleculeHSP70inducer.Neuropharmacology.2011May;60(6):991-9.McePdfHeightCaution:Producthasnotbeenfully