TD-198946-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETD-198946Cat.No.:HY-15642CASNo.:364762-86-7分⼦式:C₂₇H₂₂N₄O₃S分⼦量:482.55作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥28mg/mL(58.03mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0723mL10.3616mL20.7232mL5mM0.4145mL2.0723mL4.1446mL10mM0.2072mL1.0362mL2.0723mL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。BIOLOGICALACTIVITY⽣物活性TD-198946⼀种噻吩并唑衍⽣物。它⼀种⾼效的软⾻形成剂。体外研究TD-198946isapotentchondrogenicagent.TD-198946stronglyinduceschondrogenicdifferentiationwithoutpromotinghypertrophyincellandmetatarsalorgancultures.TD-198946inducesstrongerCol2a1promoter1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEactivitythaninsulininATDC5cells.InC3H10T1/2cells,ATDC5cellsandprimarymousechondrocytes,TD-198946dose-dependentlystimulatesendogenousexpressionofthechondrocytemarkersCol2a1andAcan,withmaximumeffectsaround1-10μM[1].体内研究Whenadministereddirectlyintothejointspace,TD-198946successfullypreventsandrepairesdegenerationofthearticularcartilage.TD-198946exertsitseffectthroughtheregulationofRunx1expression,whichisdownregulatedinbothmouseandhumanOAcartilagecomparedwithnormaltissue[1].TD-198946hasdisease-modifyingeffectsonprogressedosteoarthritis.TD-198946maypreventtheprogressionofosteoarthritisbyactingontheremainingchondrocytesratherthanrepairingdamagedcartilage,itmaybemosteffectiveasatherapeuticduringtheearlyormiddlestagesofosteoarthritis,beforethearticularcartilageisfullyeroded[2].Cartilaginouscell-sheetsaregeneratedbyculturingmouseandcaninecostalchondrocytesandhumanmesenchymalstemcellswithTD-198946ontemperature-responsivedishes.Thetransplantedcell-sheetsarethensuccessfullyusedtopromotethereconstructionofpermanentcartilage,withnoevidenceofchondrocytehypertrophyinthekneearticularcartilagedefectscreatedinmiceandcanines[3].PROTOCOLAnimalMice:Eachofthepreventionandrepairmodelshadtwogroups:(1)TD-198946-treatedanimalsand(2)Administration[1]saline-treatedanimals.Inallthemicetestedtheleftkneejointsunderwenttheoperationandtherightkneejointsaresham-operated.Micearere-anaesthetisedandgivena10µLintra-articularinjectionofTD-198946orsalineimmediatelyaftersurgery(preventionmodel)or4weeksfollowingsurgery(repairmodel)every5daysfor8or4weeks,respectively[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].YanoF,etal.Anoveldisease-modifyingosteoarthritisdrugcandidatetargetingRunx1.AnnRheumDis.2013May;72(5):748-53.[2].YanoF,etal.Disease-modifyingeffectsofTD-198946onprogressedosteoarthritisinamousemodel.AnnRheumDis.2014Nov;73(11):2062-4.[3].YanoF,etal.Cell-sheettechnologycombinedwithathienoindazolederivativesmallcompoundTD-198946forcartilageregeneration.Biomaterials.2013Jul;34(22):5581-7.[4].KobayashiM,ChijimatsuR,HartDA,etal.EvidencethatTD-198946enhancesthechondrogenicpotentialofhumansynovium-derivedstemcellsthroughtheNOTCH3signalingpathway.JTissueEngRegenMed.2021;15(2):103-115.McePdfHeightCaution:Producthasno