iGOT1-01-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEiGOT1-01Cat.No.:HY-124825CASNo.:882256-55-5分⼦式:C₁₉H₂₀N₄O分⼦量:320.39作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(312.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1212mL15.6060mL31.2120mL5mM0.6242mL3.1212mL6.2424mL10mM0.3121mL1.5606mL3.1212mL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%salineSolubility:≥2.5mg/mL(7.80mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.80mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性iGOT1-01有效的天冬氨酸转氨酶1(⾕氨酸草酰⼄酸转氨酶1；GOT1)抑制剂，在MDH偶联GOT1酶法测定中IC50为85μM，在GOT1/GLOX/HRP测定中IC50为11.3μM。iGOT1-01具有抗癌活性。IC50&TargetIC50:85μM(MDHcoupledGOT1enzymaticassay)and11.3μM(GOT1/GLOX/HRPassay)[1]体外研究iGOT1-01hasanIC50of84.6μMintheGOT1/MDH1assay.NoinhibitoryactivityisobservedforiGOT1-01againstMDH1aloneat100μM[2].iGOT1-01(3.125-200μM;for3h)revealslittletonotoxicityusingtworeadoutsofcellviabilityinPaTu8902pancreaticandDLD1coloncancercells[2].体内研究iGOT1-01(compound1a;20mg/kg;oral)hasreasonablebioavailabilityandexposureproperties(t1/2=0.7hours,Cmax=4133ng/mL,AUC(0-24hours)=11734hour•ng/mL)[1].AnimalModel:FemaleCD1micewith9weeksold[1]Dosage:20mg/kg(PharmacokineticAnalysis)Administration:OralResult:Hasreasonablebioavailabilityandexposureproperties(t1/2=0.7hours,Cmax=4133ng/mL,AUC(0-24hours)=11734hour•ng/mL).REFERENCES[1].JustinAnglin,etal.Discoveryandoptimizationofaspartateaminotransferase1inhibitorstotargetredoxbalanceinpancreaticductaladenocarcinoma.BioorgMedChemLett.2018Sep1;28(16):2675-2678.[2].MelissaCHolt,etal.BiochemicalCharacterizationandStructure-BasedMutationalAnalysisProvideInsightintotheBindingandMechanismofActionofNovelAspartateAminotransferaseInhibitors.Biochemistry.2018Nov27;57(47):6604-6614.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications