ABT-107-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEABT-107Cat.No.:HY-108038CASNo.:855291-54-2分?式:C??H??N?O分?量:320.39作?靶點(diǎn):nAChR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:100mg/mL(312.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1212mL15.6060mL31.2120mL5mM0.6242mL3.1212mL6.2424mL10mM0.3121mL1.5606mL3.1212mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.80mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.80mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性ABT-107選擇性的α7神經(jīng)元尼古丁受體的激動(dòng)劑。ABT-107對(duì)單側(cè)6-羥多巴胺損傷??的?質(zhì)紋狀體損傷起到保護(hù)作?。體內(nèi)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?邊的抑制劑?師www.MedChemE[2].TanujaBordia,etal.Theα7nicotinicreceptoragonistABT-107protectsagainstnigrostriataldamageinratswithunilateral6-hydroxydopaminelesions.ExpNeurol.2015Jan;263:277-84.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf