GSK1016790A-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK1016790ACat.No.:HY-19608CASNo.:942206-85-1分?式:C??H??Cl?N?O?S?分?量:655.61作?靶點:TRPChannel;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:≥33mg/mL(50.33mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5253mL7.6265mL15.2530mL5mM0.3051mL1.5253mL3.0506mL10mM0.1525mL0.7626mL1.5253mL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(3.81mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(3.81mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.17mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK1016790A有效的，選擇性瞬時受體電位?草酸4(TRPV4)通道激活劑。GSK1016790A可以引起HEK細胞中Ca2+流?并升?細胞內(nèi)Ca2+。IC50&TargetTRPV4體外研究GSK1016790A(0.1-1000nM)elicitsCa2+influxinmouseandhumanTRPV4-expressinghumanembryonickidney(HEK)cells(EC50valuesof18and2.1nM,respectively)anditevokesadose-dependentactivationofTRPV4whole-cellcurrentsatconcentrationsabove1nM.GSK1016790A(100nM)treatmentelicitsarapidelevationofintracellularCa2+inasubsetofneurons[2].體內(nèi)研究GSK1016790A(0.001-0.1mg/kg;i.p.)producesadose-dependentinhibitoryeffectonwholeguttransittimeinmice[2].GSK1016790A(0.1-1000nM;pretreatment10min)significantlyinhibitstheelectricalfieldstimulation(EFS)-inducedtwitchcontractionsinisolatedmousecolonstripsinaconcentration-dependentmanner[2].AnimalModel:S100β-GFPandTRPV4knockout(TRPV4-/-)mice[2]Dosage:0.001,0.01,0.1mg/kgAdministration:IP;singledoseResult:Producedadose-dependentinhibitoryeffectonwholeguttransittimeinmice.Producedadose-dependentandtime-dependentinhibitoryeffectoncolonicexpulsion.戶使?本產(chǎn)品發(fā)表的科研?獻?BrJPharmacol.2021Nov25.?Antioxidants(Basel).2022,11(12),2315.?ActaPharmacolSin.2022Sep23.?CellCalcium.2022Jun;104:102590.?FrontPharmacol.2021Jul14;12:684538.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].KevinSThorneloe,etal.N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide(GSK1016790A),anovelandpotenttransientreceptorpotentialvanilloid4chan[2].JFichna,etal.Transientreceptorpotentialvanilloid4inhibitsmousecolonicmotilitybyactivatingNO-dependententericneurotransmission.JMolMed(Berl).2015Dec;93(12):1297-309.McePdfHeightCaution:Producthasnotbeenfullyvali