Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVosoritideCat.No.:HY-P3503CASNo.:1480724-61-5Synonyms:BMN111分?式:C???H???N??O??S?分?量:4102.73Sequence:Pro-Gly-Gln-Glu-His-Pro-Asn-Ala-Arg-Lys-Tyr-Lys-Gly-Ala-Asn-Lys-Lys-Gly-Leu-Ser-Lys-Gly-Cys-Phe-Gly-Leu-Lys-Leu-Asp-

Arg-Ile-Gly-Ser-Met-Ser-Gly-Leu-Gly-Cys(Disulfidebridge:Cys

23-Cys39)SequenceShortening:PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC(Disulfidebridge:Cys23-Cys39)作?靶點(diǎn):FGFR作?通路:ProteinTyrosineKinase/RTK儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Vosoritide(BMN111)?種改良的重組CNP(C型鈉尿肽)類似物，與NPR-B(B型鈉尿肽受體)結(jié)合并降低FGFR3(成纖維細(xì)胞?長(zhǎng)因?受體3)的活性。Vosoritide可?于軟?癥和侏儒癥的研究。體外研究Vosoritide(0.1μM;1h)decreasesNPR2phosphorylationinchondrocytes[2].Vosoritide(0.1μM;6d)improveschondrocytedifferentiationandincreasestheproliferativegrowthplateareaofculturedFgfr3Y367C/+femurs[2].Vosoritide(10μM;overnight)reducesERK1/2activationinACHgrowth-platechondrocytes[3].WesternBlotAnalysis[2]CellLine:ChondrocyteculturesConcentration:0.1μMIncubationTime:1hourResult:LedtoreductioninNPR2phosphorylation.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEWesternBlotAnalysis[3]CellLine:ChondrocyteConcentration:10μMIncubationTime:OvernightResult:PreventedFGF-mediatedincreaseinERK1/2phosphorylation.體內(nèi)研究Vosoritide(subcutaneousinjection;800μg/kg;oncedaily;20d)treatmentleadstoimprovementinskeletalparametersinFgfr3gain-of-functionmutationmouse[3].AnimalModel:Fgfr3Y367C/+mice[3]Dosage:800μg/kgAdministration:Subcutaneousinjection;800μg/kg;oncedaily;20daysResult:Observedphenotypicchangesincludingflatteningoftheskull,elongationofthesnout,improvementoftheanteriorcrossbite,largerpawsanddigits,andlongerandstraightenedtibiasandfemurs.REFERENCES[1].DugganS.Vosoritide:FirstApproval.Drugs.2021Nov;81(17):2057-2062.[2].ShuhaibarLC,etal.PhosphataseinhibitionbyLB-100enhancesBMN-111stimulationofbonegrowth.JCIInsight.2021May10;6(9):e141426.[3].LorgetF,etal.EvaluationofthetherapeuticpotentialofaCNPanaloginaFgfr3mousemodelrecapitulatingachondroplasia.AmJHumGenet.2012Dec7;91(6):1108-14.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc