ACT-709478-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEACT-709478Cat.No.:HY-112723CASNo.:1838651-58-3分?式:C??H??F?N?O分?量:425.41作?靶點:CalciumChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥125mg/mL(293.83mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3507mL11.7534mL23.5067mL5mM0.4701mL2.3507mL4.7013mL10mM0.2351mL1.1753mL2.3507mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.89mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.89mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.89mM);ClearsolutionBIOLOGICALACTIVITY?物活性ACT-709478?種?服有效的，可透過?腦屏障的選擇性T型電壓門控鈣通道(T-typecalciumchannel)阻滯劑，可?于全?性癲癇的研究[1]。IC50&TargetCav1.2CaV3.1Cav3.2CaV3.32410nM(IC50)6.4nM(IC50)18nM(IC50)7.5nM(IC50)體外研究ACT-709478(Compound66b)blocksCav3.1,Cav3.2,Cav3.3,Cav1.2withIC50sof6.4,18,7.5and2410nM,respectively.ACT-709478blocksrecombinantchannelhCav3.3potentlywithmarkedvoltage-dependency(Kr≈1500nMandKi≈20nM).ACT-709478blockscurrentsthroughhKv11.1-hERGchannelswithanIC50of5.5μM[1].ACT-709478alsoinhibitsP450enzymeswithIC50sof14,15,22,25,51and52μMforCYP2C8,CYP2D6CYP2C9,CYP2C19,CYP3A4,andCYP2B6,respectively[1].體內(nèi)研究ACT-709478(Compound66b,100,300mg/kg,p.o.,12hours)potentlydecreasesthecumulativedurationofabsence-likeseizuresinmice[1].AnimalModel:MalejuvenileDBA/2Jmice(22-24daysold)[1]Dosage:100,300mg/kg,1houror3hoursbeforeexposuretothestimulus.Administration:P.O.,for12hoursResult:Decreasedthecumulativedurationofabsence-likeseizuresoverthenext12hperiodby93%.REFERENCES[1].Bezen?onO,etal.DiscoveryofaPotent,SelectiveT-typeCalciumChannelBlockerasaDrugCandidatefortheTreatmentofGeneralizedEpilepsies.JMedChem.2017Dec14;60(23):9769-9789.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F