RU-521-RU320521-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERU.521Cat.No.:HY-114180CASNo.:2262452-06-0Synonyms:RU320521分?式:C??H??Cl?N?O?分?量:415.23作?靶點(diǎn):CyclicGMP-AMPSynthase作?通路:Immunology/Inflammation儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:83.33mg/mL(200.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4083mL12.0415mL24.0830mL5mM0.4817mL2.4083mL4.8166mL10mM0.2408mL1.2042mL2.4083mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.01mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.01mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.01mM);ClearsolutionBIOLOGICALACTIVITY?物活性RU.521(RU320521)?種有效的，選擇性的環(huán)狀GMP-AMP合成酶(cGAS)抑制劑，抑制cGAS介導(dǎo)的?擾素上調(diào)。RU.521也抑制dsDNA報告因的活性，IC50為0.7μM。RU.521可以降低來?Aicardi-Goutières綜合征??模型的巨噬細(xì)胞中?擾素的組成型表達(dá)。IC50&TargetIC50:0.7μM(dsDNA)[1]體外研究RU.521(0.1nM-1000μM;72h)suppressesdsDNA-inducedsignalinginmacrophagecells[1].RU.521(0-100μM;24h)selectivelyinhibitscGAS-mediatedsignaling[1].體內(nèi)研究RU.521(5mg/kg;i.p.once)reducessymptomsfromsepsisinmice[2].AnimalModel:Male8-week-oldmalemicewithLPSinjection[2]Dosage:5mg/kgAdministration:Intraperitonealinjection;5mg/kgonceResult:Increasedcardiacfunctionandreducedtheinflammatoryresponses,oxidativestressandapoptosisinheartsofmice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemECommun.2017Sep29;8(1):750.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication