Pico145-HC-608-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPico145Cat.No.:HY-101507CASNo.:1628287-16-0Synonyms:HC-608分⼦式:C₂₃H₂₀ClF₃N₄O₅分⼦量:524.88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(190.52mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9052mL9.5260mL19.0520mL5mM0.3810mL1.9052mL3.8104mL10mM0.1905mL0.9526mL1.9052mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.76mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.76mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pico145(HC-608)⼀种⾼效的瞬时受体电位通道蛋⽩1/4/5(TRPC1/TRPC4/TRPC5)抑制剂，在细胞中，能够抑制(−)-englerinA活化的TRPC4/TRPC5通道，IC50值分别为0.349和1.3nM，对TRPC3，TRPC6，TRPV1，TRPV4，TRPA1，TRPM2和TRPM8⽆作⽤[1]。IC50&TargetIC50:0.349nM(TRPC4,cellassay),1.3nM(TRPC5,cellassay),0.03nM(TRPC4-TRPC1,cellassay),0.2nM(TRPC5-TRPC1,cellassay)[1]体外研究Pico145(Compound31,C31)isaremarkablesmall-moleculeinhibitorofTRPC1/4/5channels,inhibits(−)-englerinA-activatedTRPC4/TRPC5channels,withIC50sof0.349and1.3nMincells;Pico145showsnoeffectonTRPC3,TRPC6,TRPV1,TRPV4,TRPA1,TRPM2,TRPM8.Pico145alsoinhibitshumanTRPC4-TRPC1andTRPC5-TRPC1concatemersexpressedinHEK293Tet+cells(IC50,0.03nMand0.2nM,respectively).ThepotencyofPico145canbereducedbyincreased(−)-englerinAconcentration.Furthermore,Pico145potentlyinhibitsRPC4-TRPC1channelsactivatedbysphingosine1-phosphate(S1P),andsuppressesS1P-evokedCa2+entrythroughTRPC4-TRPC1channelswithanIC50of0.011nM.Pico145alsosensitizesEA-sensitivecancercellline(Hs578Tcells)(IC50,0.11nM).Pico145(100nM)lackseffectonstore-operatedCa2+entryandhistamine-evokedCa2+entryintoendothelialcells[1].PROTOCOLCellAssay[1]Cellsareseededat90%confluenceinto96-wellclear-bottomedpoly-d-lysine-coatedblackplatesforHEK293cellsandclear-bottomedNuncplatesforA498cells,Hs578Tcells,andHUVECs24hbeforeexperimentation.Fura-2Ca2+indicatordyeisusedtomonitorchangesinintracellularionizedCa2+concentration.Toperformtheexperiment,thecellsareincubatedfor1hwithfura-2-AM(2μM)instandardbathsolution(SBS)at37°Cinthepresenceof0.01%pluronicacid.SBScontains135mMNaCl,5mMKCl,1.2mMMgCl2,1.5mMCaCl2,8mMglucose,and10mMHepes(pHtitratedto7.4usingNaOH).Subsequently,thecellsarewashedtwicewithSBSbeforeaddingPico145orML204for30minbeforemakingCa2+measurements.Thefura-2fluorescenceisrecordedusinga96-wellfluorescenceplatereaderandtheexcitationwavelengthsof340and380nm[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•MolMetab.2022:101645.•FoodChemToxicol.2019Jul;129:281-290.•PLoSOne.2021Apr23;16(4):e0250095.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•BehavBrainRes.2022Jan18;113765.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RubaiyHN,etal.Picomolar,selective,andsubtype-specificsmall-moleculeinhibitionofTRPC1/4/5channels.JBiolChem.2017May19;292(20):8158-8173.McePdfHeightCaution: