Vadadustat-PG-1016548-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVadadustatCat.No.:HY-101277CASNo.:1000025-07-9Synonyms:PG-1016548;AKB-6548分⼦式:C₁₄H₁₁ClN₂O₄分⼦量:306.7作⽤靶点:HIF/HIFProlyl-Hydroxylase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(326.05mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2605mL16.3026mL32.6051mL5mM0.6521mL3.2605mL6.5210mL10mM0.3261mL1.6303mL3.2605mL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(8.15mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.15mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.15mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Vadadustat(PG-1016548)⼀种可滴定⼝服的缺氧诱导因⼦脯氨酰羟化酶(HIF-PH)抑制剂。Vadadustat是⼀种促红细胞⽣成剂，在动物慢性肾脏疾病模型中，有⽤于研究贫⾎的潜⼒。IC50&TargetIC50:HIF-PH[1]体外研究Vadadustatinducesendogenouserythropoietinsynthesisandenhancesironmobilization.Vadadustatiswell-toleratedinhealthyvolunteersandpatientswithchronickidneydisease,whereitincreasesreticulocytes,plasmaEPO,andHblevelsinadose-dependentmanner.TheincreaseinplasmaEPOlevelsseenwithvadadustatiscomparableinmagnitudetothatoccurringphysiologicallyatmoderatealtitudeandshowsanormaldiurnalpatternwithareturntobaselinelevelspriortothenextdose.Vadadustatimprovesironhomeostasisbydecreasinghepcidinandincreasingtransferrinlevels.once-dailyoraladministrationofvadadustat,titratedtoincreaseandmaintainHbinthetargetrange,mayprovidemultipleadvantagesoverconventionalESAs[1].Vadadustatisobservedtohaveahalf-lifeofapproximately4.5hours.Overall,patientsdemonstrateanincreaseinHblevels,from9.91g/dLatbaselineto10.54g/dLbyday29.Ferritinlevelsdecreasefrom334.1ng/mLatbaselineto271.7ng/mLbyday29[2].户使⽤本产品发表的科研⽂献•Cells.2020Nov1;9(11):2396.•JBiolChem.2021Feb8;100397.•DrugTestAnal.2020Aug27.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PergolaPE,etal.Vadadustat,anoveloralHIFstabilizer,provideseffectiveanemiatreatmentinnondialysis-dependentchronickidneydisease.KidneyInt.2016Nov;90(5):1115-1122.[2].GuptaN,etal.Hypoxia-InducibleFactorProlylHydroxylaseInhibitors:APotentialNewTreatmentforAnemiainPatientsWithCKD.AmJKidneyDis.2017Feb24.pii:S0272-6386(17)30110-5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform