Enarodustat-JTZ-951-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEnarodustatCat.No.:HY-109057CASNo.:1262132-81-9Synonyms:JTZ-951分⼦式:C₁₇H₁₆N₄O₄分⼦量:340.33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:83.33mg/mL(244.85mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9383mL14.6916mL29.3832mL5mM0.5877mL2.9383mL5.8766mL10mM0.2938mL1.4692mL2.9383mL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(6.11mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.11mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.11mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Enarodustat⼀种有效的，可⼝服的hypoxia-induciblefactorprolylhydroxylase抑制剂，EC50of0.22μM。Enarodustat有潜⼒⽤于肾性贫⾎症的研究。IC50&TargetEC50:0.22μM(factorprolylhydroxylase)[1]体外研究Enarodustat(JTZ-951)isapotentandorallyactivehypoxia-induciblefactorprolylhydroxylaseinhibitor,withanEC50of0.22μM.EnarodustatexhibitsneitherCYP(IC50>100μM;CYP3A4/5,CYP2C9,CYP2D6,CYP1A2,CYP2A6,CYP2C19,CYP2C8,CYP2B6)norhERG(IC50>100μM)inhibition[1].体内研究Enarodustat(1and3mg/kg,p.o.)increaseshemoglobinlevelsinadose-dependentmannerwithdailyoraldosinginrats[1].户使⽤本产品发表的科研⽂献•ACSOmega.August29,2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].OgoshiY,etal.DiscoveryofJTZ-951:AHIFProlylHydroxylaseInhibitorfortheTreatmentofRenalAnemia.ACSMedChemLett.2017Nov20;8(12):1320-1325.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T