TRC051384-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETRC051384Cat.No.:HY-101712CASNo.:867164-40-7分?式:C??H??N?O?分?量:465.54作?靶點(diǎn):HSP作?通路:CellCycle/DNADamage;MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(214.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1480mL10.7402mL21.4804mL5mM0.4296mL2.1480mL4.2961mL10mM0.2148mL1.0740mL2.1480mL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。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.37mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性TRC051384熱休克蛋?70(HSP70)誘導(dǎo)劑。IC50&TargetHSP70體外研究TRC051384,dosedependentlyinducesHSP70BmRNAbyseveralhundredfoldsinbothHeLaandratprimarymixedneurons.TreatmentwithTRC051384resultsinsignificantdose-dependentincreaseinHSF1transcriptionalactivityandrecoveryofluciferaseactivity.TRC051384resultsin60%inhibitionat6.25μMand90%inhibitionat12.5μMofLPS-inducedTNF-αexpressionindifferentiatedTHP-1cellline[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?DomestAnimEndocrin.2021Jan;74:106533.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].MohananA,etal.DelayedinterventioninexperimentalstrokewithTRC051384--asmallmoleculeHSP70inducer.Neuropharmacology.2011May;60(6):991-9.McePdfHeightCaution:Producthasnotbeenfully