VU0357017-hydrochloride-CID-25010775-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVU0357017hydrochlorideCat.No.:HY-19752ACASNo.:1135242-13-5Synonyms:CID-25010775分⼦式:C₁₈H₂₈ClN₃O₃分⼦量:369.89作⽤靶点:mAChR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:33.33mg/mL(90.11mM;Needultrasonic)DMSO:25mg/mL(67.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7035mL13.5175mL27.0351mL5mM0.5407mL2.7035mL5.4070mL10mM0.2704mL1.3518mL2.7035mL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(sealedstorage,awayfrommoisture)。-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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.76mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.76mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.76mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性VU0357017hydrochloride(CID-25010775)⼀种有效、选择性和可透过⾎脑屏障的M1毒蕈碱⼄酰胆碱受体变构激动剂，EC50值为477nM。VU0357017hydrochloride对M1具有⾼度选择性，在测试的最⾼浓度(30μM)下，在M2-M5处没有活性。VU0357017hydrochloride可⽤于阿尔茨海默症和精神分裂症的研究。IC50&TargetIC50:477nM(M1)[1]体外研究VU0357017isselectiveforM1(Ki=9.91µM)overM2-M5mAChRs(Ki=21.4,55.3,35.0,and50.0μM,respectively)inCHOcells[1].VU0357017(1nM-100μM)inducescalciumreleaseandERKphosphorylationinaconcentration-dependentmannerinCHOcells[3].体内研究VU0357017(1-10mg/kg,i.p.)reversesscopolamine-induceddisruptionofthecontextualfearconditioningresponse[2].AnimalModel:MaleSprague−Dawleyrats(380-420g)werepretreatedwithscopolamine[2]Dosage:1,3,10mg/kgAdministration:Asinglei.p.Result:Producedasignificantreversalofthescopolamine-induceddeficitsatadoseof10mg/kg.REFERENCES[1].DigbyGJ,etal.ChemicalmodificationoftheM(1)agonistVU0364572revealsmolecularswitchesinpharmacologyandabitopicbindingmode.ACSChemNeurosci.2012Dec19;3(12):1025-36.[2].LeboisEP,etal.Discoveryandcharacterizationofnovelsubtype-selectiveallostericagonistsfortheinvestigationofM(1)receptorfunctioninthecentralnervoussystem.ACSChemNeurosci.2010;1(2):104-121.[3].DigbyGJ,etal.NovelallostericagonistsofM1muscarinicacetylcholinereceptorsinducebrainregion-specificresponsesthatcorrespondwithbehavioraleffectsinanimalmodels.JNeurosci.2012Jun20;32(25):8532-44.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica