PAT-1251-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPAT-1251Cat.No.:HY-107422CASNo.:2007885-39-2分⼦式:C₁₈H₁₇F₄N₃O₃分⼦量:399.34作⽤靶点:MonoamineOxidase作⽤通路:NeuronalSignaling储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:≥130mg/mL(325.54mM)H2O:≥100mg/mL(250.41mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5041mL12.5207mL25.0413mL5mM0.5008mL2.5041mL5.0083mL10mM0.2504mL1.2521mL2.5041mL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(storedundernitrogen)。-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:≥2.17mg/mL(5.43mM);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:≥2.17mg/mL(5.43mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(5.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PAT-1251⼀种有效的，选择性的，可⼝服的赖氨酰氧化酶样蛋⽩2(LOXL2)抑制剂，对hLOXL2和hLOXL3的IC50值分别为0.71和1.17μM，同时对⼩⿏、⼤⿏和狗LOXL2的抑制作⽤很强，IC50值分别为0.10，0.12和0.16μM；PAT-1251可⽤于多种纤维性疾病的研究[1]。IC50&TargetIC50:0.10μM(MouseLOXL2),0.12μM(RatLOXL2),0.16μM(DogLOXL2),0.71μM(hLOXL2),1.17μM(hLOXL3)[1]体外研究PAT-1251isaLysylOxidase-Like2(LOXL2)inhibitor,withIC50sof0.71and1.17μMforhLOXL2andhLOXL3,respectively,andalsopotentlyinhibitsmouse,rat,anddogLOXL2(IC50s,0.10,0.12,and0.16μM,respectively).PAT-1251showshighlyselectiveforLOXL2overotherkeymembersoftheamineoxidasefamily,suchasthecopper-dependentamineoxidasessemicarbazide-sensitiveamineoxidase(SSAO)anddiamineoxidase(DAO),inadditiontotheflavin-dependentmonoamineoxidasesA(MAO-A)andB(MAO-B),with[1].REFERENCES[1].RowbottomMW,etal.Identificationof4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridineDerivativesasPotent,Selective,andOrallyEfficaciousInhibitorsoftheCopper-DependentAmineOxidase,LysylOxidase-Like2(LOXL2).JMedChem.2017May25McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese