Pyr10-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPyr10Cat.No.:HY-19408CASNo.:1315323-00-2分⼦式:C₁₈H₁₃F₆N₃O₂S分⼦量:449.37作⽤靶点:TRPChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(222.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2253mL11.1267mL22.2534mL5mM0.4451mL2.2253mL4.4507mL10mM0.2225mL1.1127mL2.2253mL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%salineSolubility:≥2.5mg/mL(5.56mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.56mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pyr10⼀种吡唑衍⽣物和⼀种选择性TRPC3通道抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的HEK293细胞中的Ca2+流⼊，IC50为0.72μM(对于BRL-2H3细胞中存储的Ca2+进⼊，IC50为13.08μM)。Pyr10具有区分受体操纵的TRPC3和天然质相互作⽤分⼦1(STIM1)/Orai1通道的能⼒。IC50&TargetTRPC30.72μM(IC50)体外研究Pyr10hastheabilitytodiscriminatebetweentheclassicalOrai-mediated,highlyCa2+selectivesignallingpathwayandthephospholipaseC-dependentCa2+entry-mediatedbyTRPCchannels,specificallybyTRPC3.Pyr10(3μM)completelyeliminatesTRPC3currentsaswellasCa2+entrywhileexertingmodesteffectsonOrai-mediatedresponses.TheselectiveblockofTRPC3channelsbyPyr10barelyaffectedmastcellactivation[1].体内研究Geneticdeletion(TRPC3-/-)andpharmacologicalchannelblockadewithPyr10bluntsventricularcardiacfibroblastactivationandmyocardialfibrosisinN(ω)-nitro-l-argininemethylester(l-NAME)hypertensivemice[2].户使⽤本产品发表的科研⽂献•LabInvest.2021Sep8.•JCellMolMed.2020Jan;24(1):488-510.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SchleiferH,etal.Novelpyrazolecompoundsforpharmacologicaldiscriminationbetweenreceptor-operatedandstore-operatedCa(2+)entrypathways.BrJPharmacol.2012Dec;167(8):1712-1722.[2].SalibaY,etal.TransientReceptorPotentialCanonical3andNuclearFactorofActivatedTCellsC3SignalingPathwayCriticallyRegulatesMyocardialFibrosis.AntioxidRedoxSignal.2019Jun1;30(16):1851-1879.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.