Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIcilinCat.No.:HY-11062CASNo.:36945-98-9Synonyms:AG-3-5分?式:C??H??N?O?分?量:311.29作?靶點(diǎn):TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥54mg/mL(173.47mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2124mL16.0622mL32.1244mL5mM0.6425mL3.2124mL6.4249mL10mM0.3212mL1.6062mL3.2124mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.03mM);ClearsolutionBIOLOGICALACTIVITY?物活性Icilin(AG-3-5)超強(qiáng)的瞬時(shí)受體電位M8(TRPM8)離?通道激動(dòng)劑。Icilin以劑量依賴性?式激活EGTA中的TRPM8（EC50=1.4μM。Icilin?種“超冷劑”[1][2]。Icilin通過調(diào)節(jié)T細(xì)胞反應(yīng)減輕??免疫性神經(jīng)炎癥[3]。IC50&TargetTRPM8體外研究Icilin-evokedTRPM8currentsshowvariableactivationkineticsandCa2+dependence.Icilin-evokedcurrentsexhibithighlyvariablelatencieswithpronounceddesensitization[1].CellViabilityAssay[1]CellLine:TRPM8-expressingoocytesorHEK293cellsConcentration:10μMIncubationTime:3minutesforTRPM8-expressingoocytes;1minuteforHEK293cellsResult:Activatedmembranecurrentswithvariabledelayofonsetinvoltage-clampedTRPM8-expressingoocytesorHEK293cells.體內(nèi)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?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical