AR7-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAR7Cat.No.:HY-101106CASNo.:80306-38-3分⼦式:C₁₅H₁₂ClNO分⼦量:257.71作⽤靶点:RAR/RXR作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(97.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8803mL19.4017mL38.8033mL5mM0.7761mL3.8803mL7.7607mL10mM0.3880mL1.9402mL3.8803mL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(9.70mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—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(9.70mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.70mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AR7⾮典型的RARA/RARα(视酸受体α)拮抗剂。AR7特异性激活伴侣介导的⾃噬(CMA)活性，⽽不会响⾃噬。体外研究TreatmentwithRARAantagonist,AR7(20μM;for16h),increasedlysosomalactivityinWTandLRRK2R1441GKImutantMEFs[1].AR7(10,20,30uM;12,24hours)hasnoeffectonmacroautophagyinNIH3T3cells[2].Chaperone-mediatedautophagy(CMA)contributestocellularqualitycontrolandthecellularresponsetostressthroughtheselectivedegradationofcytosolicproteinsinlysosomes.DecreaseinCMAactivityoccursinagingandinage-relateddisorders.Signalingthroughtheretinoicacidreceptoralpha(RARα)inhibitsCMA.AR7significantlyactivatesCMAactivityinmousefibroblasts.AmarkedincreaseinCMA-activatingpotencyisfoundwhenAR7andGR1arecombined,supportingtheircooperativeeffect.TreatmentwiththetranscriptionalrepressorActinomycinDpartiallyreducesthestimulatoryeffectofAR7onCMA,consistentwithtranscriptionalchangescontributingtotheupregulationofCMA[3].户使⽤本产品发表的科研⽂献•Allergy.2021Aug8.•JNeuroinflammation.2021Dec20;18(1):295.•Diabetes.2022Sep28;db220355.•BiochemBiophysResCommun.2020Jul23;528(2):276-284.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AnguianoJ,etal.Chemicalmodulationofchaperone-mediatedautophagybyretinoicacidderivatives.NatChemBiol.2013Jun;9(6):374-82.[2].PhilipWing-LokHo,etal.Age-dependentaccumulationofoligomericSNCA/α-synucleinfromimpaireddegradationinmutantLRRK2knockinmousemodelofParkinsondisease:rolefortherapeuticactivationofchaperone-mediatedautophagy(CMA).Autophagy.2020[3].MathieuBourdenx,etal.Chaperone-mediatedautophagypreventscollapseoftheneuronalmetastableproteome.Cell.2021May13;184(10):2696-2714.e25.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor