H-151-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEH-151Cat.No.:HY-112693CASNo.:941987-60-6分?式:C??H??N?O分?量:279.34作?靶點:STING作?通路:Immunology/Inflammation儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:31.25mg/mL(111.87mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.5799mL17.8993mL35.7987mL5mM0.7160mL3.5799mL7.1597mL10mM0.3580mL1.7899mL3.5799mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(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%salineSolubility:≥2.08mg/mL(7.45mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.08mg/mL(7.45mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性H-151?種有效，選擇性和共價的STING拮抗劑，在體外和體內(nèi)均具有顯的抑制活性。H-151減少TBK1磷酸化并抑制STING棕櫚?；-151可?于??炎癥性疾病的研究。IC50&TargetSTING[1]體外研究H-151(0.02-2μM)reducesIFNβluciferasereportermeasurementsofHEK293Tcells[1].H-151(0.5μM;2h)inhibitsthephosphorylationofTBK1inTHP-1cells[1].H-151(1μM;3h)suppresseshsSTINGpalmitoylation[1].體內(nèi)研究H-151(750nmolpermouse;asinglei.p.)markedlyreducessystemiccytokineresponsesinCMA-treatedmice[1].H-151(750nmolpermouse;i.p.dailyfor7d)exhibitsnotableefficacyinTrex1?/?micethatexpressedabioluminescentIFNβreporter[1].H-151(750nmolpermouse;i.p.)reacheseffectivesystemiclevels,displaysashorthalf-lifeintheserumandformsanadducttommSTINGinwild-typemice[1].戶使?本產(chǎn)品發(fā)表的科研?獻?CellMetab.2021Jul28;S1550-4131(21)00325-9.?Neuron.2022Nov4;S0896-6273(22)00961-8.?CancerRes.2021Feb15;canres.2370.2020.?ExpMolMed.2022Feb;54(2):129-142.?IntJBiolSci.2022Jan1;18(2):585-598.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HaagSM,etal.TargetingSTINGwithcovalentsmall-moleculeinhibitors.Nature.2018Jul;559(7713):269-273.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch