PPARδ-agonist-10-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPPARδagonist10Cat.No.:HY-121542CASNo.:685139-10-0分⼦式:C₂₃H₁₇Br₂ClO₃S分⼦量:568.71作⽤靶点:PPAR作⽤通路:CellCycle/DNADamage;MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PPARδagonist10(compound7)⼀种具有⼝服活性、选择性的PPARδ部分激动剂，对hPPARδ(LBD)-GAL4和mPPARδ的EC50值分别为0.053μM和0.30µM。PPARδagonist10在反式激活测定中部分PPARδ激动剂，但在体外和体内都肌⾁细胞游离脂酸氧化的完全激动剂。PPARδagonist10可⽤于⾎脂异常研究[1]。IC50&TargetPPARδPPARδ0.053μM(EC50,hPPARδ)0.30μM(EC50,mPPARδ)体外研究PPARδagonist10(compound7)increasesfattyacidoxidationinratL6musclecells,withEC50of30nM[1].体内研究PPARδagonist10(compound7)changesplasmalipidparametersinadose-dependentmannertoalessatherogenicprofile[1].PPARδagonist10(5-20mg/kg,PO,oncedaily)showsgoodoralpharmacokineticpropertiesinrat[1].AnimalModel:ApoB100/CETP-Tgnmice(female,9-11weeksold,withameanbodyweightof19.2g±1.4,n=8/group,werefedahighfatdiet)[1]Dosage:5,10,and20mg/kgAdministration:PO,oncedaily,for6weeksResult:Changedplasmalipidparametersinadose-dependentmannertoalessatherogenicprofile,withincreasedHDLanddecreasedLDLandTG.HbA1clevelswerelowered.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleSDrats[1]Dosage:1.06mg/kg(IV)/2.06mg/kg(PO)Administration:p.o.andi.v.,single(PharmacokineticAnalysis)Result:PharmacokineticParametersofPPARδagonist10inmaleSprague-Dawleyrats[1].IV(1.06mg/kg)PO(2.06mg/kg)Cmax(ng/mL)508AUC0-24(ng/mL∗min)79294t1/2(min)59CL(mL/min/kg)11.9Vd,ss(L/kg)0.3F(%)46%REFERENCES[1].SauerbergP,etal.IdentificationandsynthesisofanovelselectivepartialPPARdeltaagonistwithfullefficacyonlipidmetabolisminvitroandinvivo.JMedChem.2007Apr5;50(7):1495-503.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4