Anle138b-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAnle138bCat.No.:HY-101855CASNo.:882697-00-9分?式:C??H??BrN?O?分?量:343.17作?靶點:Amyloid-β作?通路:NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥50mg/mL(145.70mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9140mL14.5700mL29.1401mL5mM0.5828mL2.9140mL5.8280mL10mM0.2914mL1.4570mL2.9140mL請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.29mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.29mM);ClearsolutionBIOLOGICALACTIVITY?物活性Anle138b?種低聚物聚集抑(oligomericaggregation)調節(jié)劑，可阻斷朊病毒蛋?(PrPSc)和α-突觸核蛋?(α-syn)病理性聚集的形成。Anle138b在體內強烈抑制低聚物積累、神經元變性和疾病進展。Anle138b毒性低，?服?物利?度?，?腦屏障通透性好。Anle138b阻斷Aβ通道并挽救淀粉樣變性??模型的疾病表型。體外研究Oligomericaggregatesarepresumedtobethekeyneurotoxicagent.Anle138bblockstheformationofpathologicalaggregatesofprionproteinandofα-synuclein,whichisdepositedinParkinson’sdiseaseandothersynucleinopathiessuchasdementiawithLewybodiesandmultiplesystematrophy.Anle138bstronglyinhibitsallprionstrainstestedincludingBSE-derivedandhumanprions.Anle138bshowsstructure-dependentbindingtopathologicalaggregatesandstronglyinhibitsformationofpathologicaloligomersbothforprionproteinandα-synuclein[1].體內研究Anle138bshowsstructure-dependentbindingtopathologicalaggregatesandstronglyinhibitsformationofpathologicaloligomersinvitroandinvivobothforprionproteinandα-synuclein[1].Anle138b(0.6-2g/kg;p.o.)modulatesα‐synucleinoligomerization[3].AnimalModel:Two‐month‐oldPLP‐hαSynmice[3]Dosage:0.6and2g/kgAdministration:OralResult:PreventedmotordeficitsandneurodegenerationinthePLP‐hαSynmice.REFERENCES[1].WagnerJ,etal.Anle138b:anoveloligomermodulatorfordisease-modifyingtherapyofneurodegenerativediseasessuchasprionandParkinson'sdisease.ActaNeuropathol.2013Jun;125(6):795-813.[2].MartinezHernandezA,etal.Thediphenylpyrazolecompoundanle138bblocksAβchannelsandrescuesdiseasephenotypesinamousemodelforamyloidpathology.EMBOMolMed.2018;10(1):32-47.[3].Heras-GarvinA,etal.Anle138bmodulatesα-synucleinoligomerizationandpreventsmotordeclineandneurodegenerationinamousemodelofmultiplesystematrophy.MovDisord.2019;34(2):255-263.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi