Teplinovivint-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETeplinovivintCat.No.:HY-137454CASNo.:1428064-91-8分⼦式:C₂₅H₂₆N₆O₂分⼦量:442.51作⽤靶点:Wnt;β-catenin作⽤通路:StemCell/Wnt储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:83.33mg/mL(188.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2598mL11.2992mL22.5984mL5mM0.4520mL2.2598mL4.5197mL10mM0.2260mL1.1299mL2.2598mL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(4.70mM);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(4.70mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Teplinovivint⼀种有效的wnt/β-catenin信号通路抑制剂。Teplinovivint具有抗炎活性，具有⽤于肌腱病研究的潜⼒。IC50&TargetWnt体外研究Teplinovivint(compound175;0.0003-10μM)inhibitsWnt/p-cateninactivityinhumancolorectalcancecellline(SW480)inadose-dependentmanner(EC50=152.9nM)[1].TeplinovivintinhibitsSW480cells(EC50=25nM)andprimaryhumanmesenchymalstemcells(hMSCs;EC50=10.377μM)[1].Teplinovivint(5.8,10.8,21.7,41.7,83.3,166.6,333.3,750nM)inducedtheexpressionofSCXA,TenacinCandTenomodulin,inadose-dependentmannerwithanEC50between139-189nM[1].体内研究Teplinovivint(compound175;10mg/ml;oncedailyfor21daysviatopicalapplication)causesameliorationofinflammationaswellastendondegeneration.Teplinovivintresultsinadecreaseofaninflammatoryplasmabiomarker,KC/GROintheCollagenase-inducedTendonInjuryModel[1].Teplinovivint(1mg/mlwith1%BA)hasaTmaxof1hoursinplasma[1].REFERENCES[1].VishalDESHMUKH,etal.Methodsofusingindazole-3-carboxamidesandtheiruseaswnt/b-cateninsignalingpathwayinhibitors.WO2018075858A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo