KR-33493-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKR-33493Cat.No.:HY-100755CASNo.:1021497-97-1分⼦式:C₂₀H₁₈BrN₃O₃S分⼦量:460.34作⽤靶点:TNFReceptor作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥31mg/mL(67.34mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1723mL10.8615mL21.7231mL5mM0.4345mL2.1723mL4.3446mL10mM0.2172mL1.0862mL2.1723mL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(5.43mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性KR-33493⼀个有效的Fas介导细胞死亡(FAF1)的抑制剂。IC50&TargetFas体内研究BodyweightchangesofbothsexesarenotrelatedtoKR-33493inalldoses.InratsadministratedKR-33493for4weeks,notestarticle-relatedchangesinanytreatedgroupsofeithersexarefoundinhematology,serumbiochemistry,andurinalysis.IndogsadministratedKR-33493for2weeks,redbloodcellcount(RBC)valueinmalesissignificantlyhigheratthe1000mg/kg/daydosethanthatofthecontrolgroup(i.e.,6.96±0.323vs.6.12±0.418).However,thechangeofRBCisrecoveredaftertheendoftheadministrationperiod.Thedose-normalizedAUClastisnotsignificantlydifferentbetweenthegroups,suggestingthatKR-33493isgovernedbylinearkinetics[1].PROTOCOLAnimalAtotalof93maleand93femalespecificpathogen-freerats(6weeksofage),and16maleand16femaleAdministration[1]beagledogs(8monthsofage)areusedinthisstudy.Inatoxicokineticstudy,ratbloodsamples(approximately0.6mL)arecollectedintotubescontainingheparinfromthelateraltailveinat0,0.5,1,2,4,8,12,and24hafterdosingwithKR-33493atdosesof50,150,and500mg/kg/dayonDay1andWeek4.Dogbloodsamples(approximately0.6mL)arecollectedintotubescontainingEDTA-2Kfromthecephalicveinat0,0.5,1,2,4,6,8,and24hafterdosingatKR-33493dosesof50,250,and1000mg/kg/dayonDay1andWeek2.Theplasmaisseparatedbycentrifugation(approximately132,000g,3min,4°C)andstoredatapproximately-80°Cuntilanalysis.TheKR-33493concentrationinplasmaisquantified[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].JeongJW,etal.SubacutetoxicityevaluationofKR-33493,FAF1inhibitorforanewanti-parkinson'sdiseaseagent,afteroraladministrationinratsanddogs.RegulToxicolPharmacol.2016Nov;81:387-396.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo