PAT-1251-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPAT-1251Cat.No.:HY-107422CASNo.:2007885-39-2分?式:C??H??F?N?O?分?量:399.34作?靶點(diǎn):MonoamineOxidase作?通路:NeuronalSignaling儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥130mg/mL(325.54mM)H2O:≥100mg/mL(250.41mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5041mL12.5207mL25.0413mL5mM0.5008mL2.5041mL5.0083mL10mM0.2504mL1.2521mL2.5041mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.17mg/mL(5.43mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.17mg/mL(5.43mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(5.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性PAT-1251?種有效的，選擇性的，可?服的賴氨酰氧化酶樣蛋?2(LOXL2)抑制劑，對(duì)hLOXL2和hLOXL3的IC50值分別為0.71和1.17μM，同時(shí)對(duì)??、??和狗LOXL2的抑制作?很強(qiáng)，IC50值分別為0.10，0.12和0.16μM；PAT-1251可?于多種纖維性疾病的研究[1]。IC50&TargetIC50:0.10μM(MouseLOXL2),0.12μM(RatLOXL2),0.16μM(DogLOXL2),0.71μM(hLOXL2),1.17μM(hLOXL3)[1]體外研究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