Seralutinib-GB002-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESeralutinibCat.No.:HY-109190CASNo.:1619931-27-9Synonyms:GB002;PK10571分⼦式:C₂₇H₂₇N₅O₃分⼦量:469.53作⽤靶点:PDGFR作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(212.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1298mL10.6489mL21.2979mL5mM0.4260mL2.1298mL4.2596mL10mM0.2130mL1.0649mL2.1298mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.32mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5.75mg/mL(12.25mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.32mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Seralutinib(GB002)⼀个可吸⼊的PDGFRα和PDGFRβ激酶抑制剂。Seralutinib(GB002)可⽤于肺动脉⾼压的研究。体内研究Seralutinib(GB002)(two-weektreatment,deliveredbyinhalation)significantlyreducesrightventricularsystolicpressureandmeanpulmonaryarterypressure.HemodynamicchangesareaccompaniedbyreducedpulmonaryarteriolemuscularizationandrestorationofBMPR2proteinexpressioninthelunglobesinSeralutinib(GB002)-treatedanimals.Seralutinib(GB002)iswelltolerated[1].GB002-mediatedinhibitionoflungPDGFRα/βphosphorylationinhealthySpragueDawleyratsimmediatelypostinhalation[2].GB002dose-andtime-dependentlyinduceslungBMPR2proteinexpression[2].REFERENCES[1].AnnaGalkin,etal.Abstract11102:Gb002,ANovelInhaledPdgfrKinaseInhibitor,DemonstratesEfficacyintheSu5416HypoxiaRatModelofPulmonaryArterialHypertension(pah).Circulation.2019;140:A11102.[2].AnnaGalkin,etal.PharmacologicCharacterizationofGB002,aNovelInhaledPDGFRKinaseInhibitorinDevelopmentforPulmonaryArterialHypertension(PAH).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu