H-151-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEH-151Cat.No.:HY-112693CASNo.:941987-60-6分⼦式:C₁₇H₁₇N₃O分⼦量:279.34作⽤靶点:STING作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:31.25mg/mL(111.87mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5799mL17.8993mL35.7987mL5mM0.7160mL3.5799mL7.1597mL10mM0.3580mL1.7899mL3.5799mL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%salineSolubility:≥2.08mg/mL(7.45mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.08mg/mL(7.45mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性H-151⼀种有效，选择性和共价的STING拮抗剂，在体外和体内均具有显的抑制活性。H-151减少TBK1磷酸化并抑制STING棕榈酰化。H-151可⽤于⾃⾝炎症性疾病的研究。IC50&TargetSTING[1]体外研究H-151(0.02-2μM)reducesIFNβluciferasereportermeasurementsofHEK293Tcells[1].H-151(0.5μM;2h)inhibitsthephosphorylationofTBK1inTHP-1cells[1].H-151(1μM;3h)suppresseshsSTINGpalmitoylation[1].体内研究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].户使⽤本产品发表的科研⽂献•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