PDE4-IN-12-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPDE4-IN-12Cat.No.:HY-151174分⼦式:C₃₄H₃₅NO₆分⼦量:553.64作⽤靶点:Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PDE4-IN-12⼀种强效的PDE4泛型抑制剂，其对PDE4和PDE7的IC50值分别为3.5和15nM(SI分别为2.71和4.27)。PDE4-IN-12具有较好的安全性，可⽤于炎症性肠病(IBDs)的研究。IC50&TargetPDE4D2PDE4B2PDE5A1PDE7A3.51nM(IC50)9.51nM(IC50)1.24μM(IC50)15nM(IC50)PDE10APDE8A11.02μM(IC50)194nM(IC50)体外研究PDE4-IN-12(compound22d)(10,20µM;24h)reducesthereleaseofNOinLPSinducedinflammationcellmodel(indicatesanti-inflammatoryeffect)[1].CellViabilityAssay[1]CellLine:Raw264.6cellsConcentration:10,20µMIncubationTime:24hResult:ReducedtheNOreleasebydose-dependentmannerintheLPSinducedinflammatorycellmodel.体内研究PDE4-IN-12(5mg/kg;i.p.;twicedailyfor8days)amelioratesmouseacutecolitisinducedbyDSS(dextransulfatesodium)[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEPDE4-IN-12(10mg/kg;p.o.;single)showswelltoleratedindogs[1].PDE4-IN-1(2.5mg/kg;i.v.;single)showsgreatplasmaexposure,withT1/2andAUC0-24hvaluesof4.18hand6522hng/mL[1].AnimalModel:MaleC57BL/6mice(5to6-weekold;15-17g;DSS-inducedmousemodel)[1].Dosage:5mg/kgAdministration:Intraperitonealinjection;twicedailyfor8days.Result:Amelioratedtheacutecolitisbydecreasingdiseaseactivityindex,increasingthecolonlength,andalsoamelioratingthepathologicaldamages.AnimalModel:Beagledogs[1].Dosage:10mg/kg(solvedin0.5%CMC-Nasolution).Administration:Oraladministration;single.Result:Exhibitedgoodsafety,whichcausednoemesisonbeagledogsat10mg/kg.AnimalModel:MaleC57BL/6mice(5to6-weekold;15-17g)[1].

Dosage:2.5mg/kgAdministration:Intravenousinjection;single.Result:1.19PharmacokineticParametersofPDE4-IN-12inMaleC57BL/6mice[1].T1/2(h)AUC0-24h(h⋅ng/mL)MRT0-24h(h)CL(mL/min/kg)Vss(mL/kg)IV(2.5mg/kg)4.1865221.766.40673REFERENCES[1].LiuH,etal.DiscoveryofnovelPDE4inhibitorstargetingtheM-pocketfromnaturalmangostaninwithimprovedsafetyforthetreatmentofInflammatoryBowelDiseases.EurJMedChem.2022Aug9;242:114631.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear