Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPico145Cat.No.:HY-101507CASNo.:1628287-16-0Synonyms:HC-608分?式:C??H??ClF?N?O?分?量:524.88作?靶點:TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:≥100mg/mL(190.52mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9052mL9.5260mL19.0520mL5mM0.3810mL1.9052mL3.8104mL10mM0.1905mL0.9526mL1.9052mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.76mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.76mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pico145(HC-608)?種?效的瞬時受體電位通道蛋?1/4/5(TRPC1/TRPC4/TRPC5)抑制劑，在細胞中，能夠抑制(?)-englerinA活化的TRPC4/TRPC5通道，IC50值分別為0.349和1.3nM，對TRPC3，TRPC6，TRPV1，TRPV4，TRPA1，TRPM2和TRPM8?作?[1]。IC50&TargetIC50:0.349nM(TRPC4,cellassay),1.3nM(TRPC5,cellassay),0.03nM(TRPC4-TRPC1,cellassay),0.2nM(TRPC5-TRPC1,cellassay)[1]體外研究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.戶使?本產品發表的科研?獻?MolMetab.2022:101645.?FoodChemToxicol.2019Jul;129:281-290.?PLoSOne.2021Apr23;16(4):e0250095.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?BehavBrainRes.2022Jan18;113765.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RubaiyHN,etal.Picomolar,selective,andsubtype-specificsmall-moleculeinhibitionofTRPC1/4/5channels.JBiolChem.2017May19;292(20):8158-8173.McePdfHeightCaution: