Anle138b-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnle138bCat.No.:HY-101855CASNo.:882697-00-9分⼦式:C₁₆H₁₁BrN₂O₂分⼦量:343.17作⽤靶点:Amyloid-β作⽤通路:NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(145.70mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9140mL14.5700mL29.1401mL5mM0.5828mL2.9140mL5.8280mL10mM0.2914mL1.4570mL2.9140mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.29mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.29mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Anle138b⼀种低聚物聚集抑(oligomericaggregation)调节剂，可阻断朊病毒蛋⽩(PrPSc)和α-突触核蛋⽩(α-syn)病理性聚集的形成。Anle138b在体内强烈抑制低聚物积累、神经元变性和疾病进展。Anle138b毒性低，⼝服⽣物利⽤度⾼，⾎脑屏障通透性好。Anle138b阻断Aβ通道并挽救淀粉样变性⼩⿏模型的疾病表型。体外研究Oligomericaggregatesarepresumedtobethekeyneurotoxicagent.Anle138bblockstheformationofpathologicalaggregatesofprionproteinandofα-synuclein,whichisdepositedinParkinson’sdiseaseandothersynucleinopathiessuchasdementiawithLewybodiesandmultiplesystematrophy.Anle138bstronglyinhibitsallprionstrainstestedincludingBSE-derivedandhumanprions.Anle138bshowsstructure-dependentbindingtopathologicalaggregatesandstronglyinhibitsformationofpathologicaloligomersbothforprionproteinandα-synuclein[1].体内研究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