CaCCinh-A01-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECaCCinh-A01Cat.No.:HY-100611CASNo.:407587-33-1分?式:C??H??NO?S分?量:347.43作?靶點:ChlorideChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥50mg/mL(143.91mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8783mL14.3914mL28.7828mL5mM0.5757mL2.8783mL5.7566mL10mM0.2878mL1.4391mL2.8783mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(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(7.20mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.20mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.20mM);ClearsolutionBIOLOGICALACTIVITY?物活性CaCCinh-A01TMEM16A和鈣激活氯化物通道(CaCC)的抑制劑，IC50值分別為2.1和10μM。IC50&TargetIC50:2.1μM(TMEM16A)[1],10μM(CaCC)[2]體外研究30μMCaCCinh-A01and100μMtannicacidstronglyinhibitCaCCcurrentfollowingATPstimulation[1].Calcium-dependentchloridecurrentisreducedby38±14,66±10,and91±1%by0.1,1,and10μMCaCCinh-A01,respectively.ATP-inducedshort-circuitcurrentsarereducedby38±7and78±3%at10and30μMCaCCinh-A01,respectively[2].體內(nèi)研究CaCCinh-A01(veininjection;5mg/kg;caudalveininjectionwithin15minaftertheonsetofreperfusion)significantlyreducesinfarctionwhencomparedwithMCAO-salinetreatmentat24hor72hinmiddlecerebralarteryocclusionmodelinmice[3].AnimalModel:Two-month-oldmaleC57/BL6Jmice[3]Dosage:5mg/kgAdministration:Veininjection;5mg/kg;caudalveininjectionwithin15minaftertheonsetofreperfusionResult:Attenuatedbraininfarctsize,improvedneurologicaloutcomesandloweredBBBpermeabilityafterischemicstrokeinmice.戶使?本產(chǎn)品發(fā)表的科研?獻?BrJPharmacol.2021Dec27.?BiochemPharmacol.2020Aug;178:114062.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TMEM16AinhibitorsrevealTMEM16Aasaminorcomponentofcalcium-activatedchloridechannelconductanceinairwayandintestinalepithelialcells.JBiolChem.2011Jan21;286(3):2365-74.[2].DeLaFuenteR,etal.Small-moleculescreenidentifiesinhibitorsofahumanintestinalcalcium-activatedchloridechannel.MolPharmacol.2008Mar;73(3):758-68.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[3].Pin-YiLiu,etal.TMEM16AInhibitionPreservesBlood-BrainBarrierIntegrityAfterIschemicStroke.FrontCellNeurosci.2019Aug6;13:360.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform