RU-521-RU320521-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERU.521Cat.No.:HY-114180CASNo.:2262452-06-0Synonyms:RU320521分⼦式:C₁₉H₁₂Cl₂N₄O₃分⼦量:415.23作⽤靶点:CyclicGMP-AMPSynthase作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:83.33mg/mL(200.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4083mL12.0415mL24.0830mL5mM0.4817mL2.4083mL4.8166mL10mM0.2408mL1.2042mL2.4083mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.01mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.01mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.01mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性RU.521(RU320521)⼀种有效的，选择性的环状GMP-AMP合成酶(cGAS)抑制剂，抑制cGAS介导的⼲扰素上调。RU.521也抑制dsDNA报告因的活性，IC50为0.7μM。RU.521可以降低来⾃Aicardi-Goutières综合征⼩⿏模型的巨噬细胞中⼲扰素的组成型表达。IC50&TargetIC50:0.7μM(dsDNA)[1]体外研究RU.521(0.1nM-1000μM;72h)suppressesdsDNA-inducedsignalinginmacrophagecells[1].RU.521(0-100μM;24h)selectivelyinhibitscGAS-mediatedsignaling[1].体内研究RU.521(5mg/kg;i.p.once)reducessymptomsfromsepsisinmice[2].AnimalModel:Male8-week-oldmalemicewithLPSinjection[2]Dosage:5mg/kgAdministration:Intraperitonealinjection;5mg/kgonceResult:Increasedcardiacfunctionandreducedtheinflammatoryresponses,oxidativestressandapoptosisinheartsofmice.户使⽤本产品发表的科研⽂献•Neuron.2022Nov4;S0896-6273(22)00961-8.•ProcNatlAcadSciUSA.2022Oct25;119(43):e2207280119.•Mbio.2021Oct12;e0240821.•CellDeathDiscov.2022May11;8(1):258.•ExpNeurol.2022:114269Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XuQ,etal.SmallmoleculeinhibitionofcyclicGMP-AMPsynthaseamelioratessepsis-inducedcardiacdysfunctioninmice.LifeSci.2020Nov1;260:118315.[2].VincentJ,etal.SmallmoleculeinhibitionofcGASreducesinterferonexpressioninprimarymacrophagesfromautoimmunemice.Nat2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECommun.2017Sep29;8(1):750.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication