OATD-01-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOATD-01Cat.No.:HY-137464ACASNo.:2088453-21-6分?式:C??H??ClN?O分?量:390.91作?靶點:Others作?通路:Others儲存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(255.81mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5581mL12.7907mL25.5813mL5mM0.5116mL2.5581mL5.1163mL10mM0.2558mL1.2791mL2.5581mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.40mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.40mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性OATD-01?種?效、?服活性、first-in-class、選擇性?丁質酶(chitinase)抑制劑，對CHIT1具有低納摩爾活性(hCHIT1,IC50=23nM)。OATD-01在多個物種中顯?出良好的藥代動?學特征。OATD-01在體內(nèi)具有顯著的抗纖維化活性，?于肺纖維化(IPF)研究。體外研究OATD-01exhibitshighaffinitytowardh/mCHIT1andh/mAMCase,andtheinhibitoryconstants(Ki)forallfourenzymesare17.3nM,26.05nM,4.8nMand5.7nM,respectively[1].TheseKivaluesrevealsgoodcorrelationwithearlierestablishedIC50data,theIC50valuesare23nM,28nM,9nMand7.8nMforhCHIT1,mCHIT1,hAMCaseandmAMCase,respectively.[1].Off-targetinvitroeffectsofcompoundOATD-01havebeenevaluatedat10μMintheEurofinsPanlabspanelof98invitrobindingandenzymaticassays,involvingdiversemolecularclassesofproteins[1].體內(nèi)研究OATD-01(oralgavage;30mg/kg,100mg/kg;oncedaily;21days)showssignificantantifibroticefficacyinananimalmodelofbleomycin-inducedpulmonaryfibrosis.Itreducesthedegreeoflungfibrosisinadose-dependentmanner,ultimatelyachievingcomparabletherapeuticefficacytoreferencetreatmentwithNintedanibinthisanimalmodel[1].AnimalModel:FemaleBALB/cmice[1]Dosage:30mg/kg,100mg/kgAdministration:Oralgavage;30mg/kg,100mg/kg;oncedaily;21daysResult:Reducedthedegreeoflungfibrosisinvivo[1]戶使?本產(chǎn)品發(fā)表的科研?獻?NeurosciRes.2021Jun7;S0168-0102(21)00121-8.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RobertKoralewski,etal.DiscoveryofOATD-01,aFirst-in-ClassChitinaseInhibitorasPotentialNewTherapeuticsforIdiopathicPulmonaryFibrosis.JMedChem.2020Dec24;63(24):15527-15540.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic