Icilin-AG-3-5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIcilinCat.No.:HY-11062CASNo.:36945-98-9Synonyms:AG-3-5分⼦式:C₁₆H₁₃N₃O₄分⼦量:311.29作⽤靶点:TRPChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥54mg/mL(173.47mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2124mL16.0622mL32.1244mL5mM0.6425mL3.2124mL6.4249mL10mM0.3212mL1.6062mL3.2124mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.03mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Icilin(AG-3-5)超强的瞬时受体电位M8(TRPM8)离⼦通道激动剂。Icilin以剂量依赖性⽅式激活EGTA中的TRPM8（EC50=1.4μM。Icilin⼀种“超冷剂”[1][2]。Icilin通过调节T细胞反应减轻⾃⾝免疫性神经炎症[3]。IC50&TargetTRPM8体外研究Icilin-evokedTRPM8currentsshowvariableactivationkineticsandCa2+dependence.Icilin-evokedcurrentsexhibithighlyvariablelatencieswithpronounceddesensitization[1].CellViabilityAssay[1]CellLine:TRPM8-expressingoocytesorHEK293cellsConcentration:10μMIncubationTime:3minutesforTRPM8-expressingoocytes;1minuteforHEK293cellsResult:Activatedmembranecurrentswithvariabledelayofonsetinvoltage-clampedTRPM8-expressingoocytesorHEK293cells.体内研究IcilinisatransientreceptorpotentialcationchannelsubfamilyM(TRPM8)agonistthatproducesbehavioralactivationinratsandmice.Icilin(3mg/kg;s.c.)induces“Wetdogshake”inmice[2].AnimalModel:TheC57BL/6mice9–10weeks(adult,26-30g)or24months(aged,35-42g)[2].Dosage:3mg/kgAdministration:Injecteds.c.Result:Producedvividandquantifiableshakingbehaviors(“wet-dogshakes”),whichwereTRPM8-dependent.REFERENCES[1].Huai-huChuang,etal.Thesuper-coolingagenticilinrevealsamechanismofcoincidencedetectionbyatemperature-sensitiveTRPchannel.Neuron.2004Sep16;43(6):859-69.[2].ViktorVFeketa,etal.Transientreceptorpotentialmelastatin8channelinhibitionpotentiatesthehypothermicresponsetotransientreceptorpotentialvanilloid1activationintheconsciousmouse.CritCareMed.2014May;42(5):e355-63.[3].BenjaminWEwanchuk,etal.ThecoolingcompoundicilinattenuatesautoimmuneneuroinflammationthroughmodulationoftheT-cellresponse.FASEBJ.2018Mar;32(3):1236-1249.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical