IDO5L-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIDO5LCat.No.:HY-15683CASNo.:914471-09-3分⼦式:C₉H₇ClFN₅O₂分⼦量:271.64作⽤靶点:Indoleamine2,3-Dioxygenase(IDO)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:≥52mg/mL(191.43mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.6813mL18.4067mL36.8134mL5mM0.7363mL3.6813mL7.3627mL10mM0.3681mL1.8407mL3.6813mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(9.20mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.20mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.20mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性IDO5L⼀种有效的吲哚胺-2,3-双加氧酶(IDO)抑制剂，IC50为67nM。IC50&TargetIDOIDO67nM(IC50)19nM(IC50,inHeLacell)体外研究IDO5L(Compound5l)isapotent(HeLaIC50=19nM)inhibitorofIDO[1].IDO5LisoneofthehighestpotentinhibitorsoftheIDO1(IC50=19nM,inHeLacellassay)[2].体内研究TestingofIDO5LinmicedemonstratespharmacodynamicinhibitionofIDO,asmeasuredbydecreasedkynureninelevels(>50%)inplasmaanddosedependentefficacyinmicebearingGM-CSF-secretingB16melanomatumors.InitialoralpharmacokineticstudiesshowthatIDO5Lisrapidlycleared(t1/250(PBadjIC50=1.0μM,murinecellularB16IC50=46nM).Notably,kynureninelevelsincreasebacktobaselineafter4hasIDO5LexposurelevelsdecreasedbelowthemousePBadjIC50from1.0to0.1μM[1].PROTOCOLAnimalMice[1]Administration[1]Asinglesubcutaneous100mg/kgdoseofIDO5LisadministeredtonaiveC57BL/6micebearingGM-CSF-secretingB16tumors.Bloodisharvestedfromindividualmiceover8h.KynurenineandIDO5LconcentrationsaremeasuredbyLCMS.Reductionsofkynureninelevelsby50-60%areobservedbetween2and4h,withmaximuminhibitionseenat2.5h.Tumorsareallowedtogrowuntilday7when14daysofsubcutaneousdosingofIDO5Lat25,50,and75mg/kgb.i.d.isinitiated.DosedependentinhibitionoftumorgrowthiscorrelatedwithincreasingexposuresofIDO5Linplasma.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•ChemSci.2020,11,7429-7437.•ChemCommun(Camb).2020Jan30;56(9):1389-1392.•Pharmaceuticals.2022,15(9),1090.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].YueEW,etal.Discoveryofpotentcompetitiveinhibitorsofindoleamine2,3-dioxygenasewithinvivopharmacodynamicactivityandefficacyinamousemelanomamodel.JMedChem.2009Dec10;52(23):7364-7.[2].HuangX,etal.Synthesisof[(18)F]4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide(IDO5L):anovelpotentialPETprobeforimagingofIDO1expression.JLabelledCompRadiopharm.2015Apr;58(4):156-62.McePdfHeightCaution:Producthasnotbe