ABT-107-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEABT-107Cat.No.:HY-108038CASNo.:855291-54-2分⼦式:C₁₉H₂₀N₄O分⼦量:320.39作⽤靶点:nAChR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:100mg/mL(312.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1212mL15.6060mL31.2120mL5mM0.6242mL3.1212mL6.2424mL10mM0.3121mL1.5606mL3.1212mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.80mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.80mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ABT-107选择性的α7神经元尼古丁受体的激动剂。ABT-107对单侧6-羟多巴胺损伤⼤⿏的⿊质纹状体损伤起到保护作⽤。体内研究ABT-107exhibitsgoodbioavailabilityinmouse(orally,51.1%;intraperitoneally,100%),rat(orally,81.2%;intraperitoneally,100.0%),andmonkey(orally,40.6%;intramuscularly,100%),andgoodCNSpenetrationinrodentswithabrain/plasmaratioof1[1].ABT-107(0.01-1μmol/kgi.p.,15minbeforesacrifice)producesadose-dependentincreaseinERK1/2andCREB[1].ABT-107(0.01,0.1,and1.0mg/kgi.p.)increasesS9-GSK3anddecreasesp-tauinmousecortexandhippocampusinmice[1].ABT-107(5mg/kg/dayi.p.)infusionattenuatestauhyperphosphorylationinADtransgenicAPP-taumice[1].AnimalModel:Rats(maleSprague-Dawley;350-380gb.wt.)[1].Dosage:1,3μmol/kg.Administration:I.P.dailyfor3consecutivedays.Result:Inducedasignificant,dose-dependentincreaseinAChreleasebyday3ofrepeatedadministration.HigherdosesmayberequiredtoevokeAChreleaseinnaiveratsnotengagedinstimulated,i.e.,cognitive-relatedbehavior.AnimalModel:FemaleTAPP(andwild-typelittermates)mice[1].Dosage:1mg/kg.Administration:Continuoussubcutaneousinfusionfor2weeks.Result:Producedadose-dependentincreaseinSer9phosphorylationinthecingulatecortex15minafteracuteadministrationinmice.REFERENCES[1].RScottBitner,etal.Invivopharmacologicalcharacterizationofanovelselectivealpha7neuronalnicotinicacetylcholinereceptoragonistABT-107:preclinicalconsiderationsinAlzheimer'sdisease.JPharmacolExpTher.2010Sep1;334(3):875-86.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].TanujaBordia,etal.Theα7nicotinicreceptoragonistABT-107protectsagainstnigrostriataldamageinratswithunilateral6-hydroxydopaminelesions.ExpNeurol.2015Jan;263:277-84.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf