CaCCinh-A01-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECaCCinh-A01Cat.No.:HY-100611CASNo.:407587-33-1分⼦式:C₁₈H₂₁NO₄S分⼦量:347.43作⽤靶点:ChlorideChannel作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(143.91mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8783mL14.3914mL28.7828mL5mM0.5757mL2.8783mL5.7566mL10mM0.2878mL1.4391mL2.8783mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.20mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.20mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.20mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CaCCinh-A01TMEM16A和钙激活氯化物通道(CaCC)的抑制剂，IC50值分别为2.1和10μM。IC50&TargetIC50:2.1μM(TMEM16A)[1],10μM(CaCC)[2]体外研究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].体内研究CaCCinh-A01(veininjection;5mg/kg;caudalveininjectionwithin15minaftertheonsetofreperfusion)significantlyreducesinfarctionwhencomparedwithMCAO-salinetreatmentat24hor72hinmiddlecerebralarteryocclusionmodelinmice[3].AnimalModel:Two-month-oldmaleC57/BL6Jmice[3]Dosage:5mg/kgAdministration:Veininjection;5mg/kg;caudalveininjectionwithin15minaftertheonsetofreperfusionResult:Attenuatedbraininfarctsize,improvedneurologicaloutcomesandloweredBBBpermeabilityafterischemicstrokeinmice.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师www.MedChemE[3].Pin-YiLiu,etal.TMEM16AInhibitionPreservesBlood-BrainBarrierIntegrityAfterIschemicStroke.FrontCellNeurosci.2019Aug6;13:360.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform