Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAR7Cat.No.:HY-101106CASNo.:80306-38-3分?式:C??H??ClNO分?量:257.71作?靶點(diǎn):RAR/RXR作?通路:MetabolicEnzyme/Protease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:25mg/mL(97.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.8803mL19.4017mL38.8033mL5mM0.7761mL3.8803mL7.7607mL10mM0.3880mL1.9402mL3.8803mL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(9.70mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—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(9.70mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.70mM);ClearsolutionBIOLOGICALACTIVITY?物活性AR7?典型的RARA/RARα(視酸受體α)拮抗劑。AR7特異性激活伴侶介導(dǎo)的?噬(CMA)活性，?不會(huì)響?噬。體外研究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].戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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