Vamorolone-VBP15-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVamoroloneCat.No.:HY-109017CASNo.:13209-41-1Synonyms:VBP15分⼦式:C₂₂H₂₈O₄分⼦量:356.46作⽤靶点:GlucocorticoidReceptor;MineralocorticoidReceptor;NF-κB作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(175.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8054mL14.0268mL28.0536mL5mM0.5611mL2.8054mL5.6107mL10mM0.2805mL1.4027mL2.8054mL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:≥2.08mg/mL(5.84mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.84mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.84mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Vamorolone(VBP15)⾸创的，具有⼝服活性的解离性类醇(dissociativesteroidal)抗炎药和膜稳定剂。Vamorolone改肌营养不良，⽆副作⽤。Vamorolone抑制(NF-κB)抑制作⽤，并降低了激素的响。体外研究Vamorolone(VBP15)inhibitsTNFα-inducedpro-inflammatoryNF-κBsignalinginC2C12musclecellsat1nMormore.Vamorolonebindstheglucocorticoidreceptor(GR)andmineralocorticoidreceptor(MR)withsimilaraffinity[1].Vamorolone(0.1,1μM;30minutes)reducesproductionofIL1βandCCL5inflammatorymediatorsinprimaryhumanmacrophages[2].Vamoroloneisafirst-in-classmineralocorticoidreceptor(MR)antagonist/dissociativeglucocorticoidreceptor(GR)ligand[3].体内研究Vamorolone(5-30mg/kg;cherrysyrup)showsasuperiorsideeffectprofilecomparedtopharmacologicalglucocorticoidsinmdxmice[1].Vamorolone(30mg/kg;orally;dailyfor20days)reducesCNSInflammationinmurineexperimentalautoimmuneencephalomyelitis[2].AnimalModel:C57BL/6mice(experimentalautoimmuneencephalomyelitis)[2]Dosage:30mg/kgAdministration:Orally;dailyfor20days(startingonedaypriortoMOG33-55peptideimmunizationandcontinuing)Result:ReducedCNSinflammationinmurineexperimentalautoimmuneencephalomyelitis.REFERENCES[1].HeierCR,etal.VBP15,anovelanti-inflammatoryandmembrane-stabilizer,improvesmusculardystrophywithoutsideeffects.EMBOMolMed.2013Oct;5(10):1569-85.[2].DillinghamBC,etal.VBP15,anovelanti-inflammatory,iseffectiveatreducingtheseverityofmurineexperimentalautoimmuneencephalomyelitis.CellMolNeurobiol.2015Apr;35(3):377-387.[3].HeierCR,etal.Vamorolonetargetsdualnuclearreceptorstotreatinflammationanddystrophiccardiomyopathy.LifeSciAlliance.2019Feb11;2(1).pii:e201800186.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidated