Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUCB-5307Cat.No.:HY-147045CASNo.:1515887-44-1分?式:C??H??N?O分?量:343.42作?靶點:TNFReceptor作?通路:Apoptosis儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數據體外實驗DMSO:50mg/mL(145.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9119mL14.5594mL29.1189mL5mM0.5824mL2.9119mL5.8238mL10mM0.2912mL1.4559mL2.9119mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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%salineSolubility:≥2.5mg/mL(7.28mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.28mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.28mM);ClearsolutionBIOLOGICALACTIVITY?物活性UCB-5307?種TNF抑制劑，對?TNFα的KD為9nM。UCB-5307可以穿透預制的hTNF/hTNFR1復合物。體外研究UCB-5307inhibitswild-typeTNFbutdoesnotinhibitL57FTNF.TheT1/2ofUCB-5307is3.3h[1].UCB-5307disruptsapreformedhTNF/hTNFR1complex,canpenetratethepreformedcomplex,dislodgingoneofthereceptors.PreloadinghTNFwithUCB-5307blocksonereceptorfrombinding[1].UCB-5307bindstoapocketinthecentreoftheTNFtrimerformedbythemovementoftheTNFmonomers,stabilisingthedistortedtrimer,whichleadstoreducedsignallingthroughTNFR1[1].REFERENCES[1].O'ConnellJ,etal.SmallmoleculesthatinhibitTNFsignallingbystabilisinganasymmetricformofthetrimer.NatCommun.2019Dec19;10(1):5795.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4