PD-166793-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesPD-166793Cat.No.:HY-107428CASNo.:199850-67-4分?式:C??H??BrNO?S分?量:412.3作?靶點(diǎn):MMP作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY?物活性PD-166793?種有效，選擇性和具有?服活性的MMP的?譜抑制劑，對(duì)MMP-2，MMP-3和MMP-13表現(xiàn)出納爾濃度的效價(jià)(IC50=4，7，8nM)，對(duì)MMP-1，-7和-9表現(xiàn)出微爾的效價(jià)(IC50=6.0，7.2，7.9μM)。PD-166793可以減輕進(jìn)?性??衰竭的??模型中的左?室重構(gòu)和功能障礙。IC50&TargetMMP-2MMP-3MMP-13MMP-14nM(IC50)7nM(IC50)8nM(IC50)6.0μM(IC50)MMP-7MMP-97.2μM(IC50)7.9μM(IC50)體外研究PD-166793(0.1μM)leadstoa20%inhibitionofAMPdeaminase(AMPD)activityinrathearthomogenates[2].PD-166793(100μM;36h)significantlyreducesMMP‐9activityinnormalhumancardiacfibroblasts[2].體內(nèi)研究PD-166793(1mg/kg/d;dailygavagefor10weeks)largelypreventstheadverseremodelingcharacteristicallyseenintheaortocaval(AV)fistulamodel[3].PD-166793(5mg/kg;oralgavage)exhibitssuperiorpharmacokinetics(t1/2=43.6h,Cmax=42.4μg/mL,AUC0-∞=2822μg?h/mL)inrats[1].AnimalModel:MaleSprague-Dawleyrats(6weeks)wereinducedchronicbiventricularvolumeoverload[3]Dosage:1mg/kg1/2Administration:Dailygavagebeginning2weeksbeforesurgeryandcontinueduntil8weeksaftersurgeryResult:Preventedventriculardilatationandattenuatedthehypertrophytypicallyinducedbychronicvolumeoverload.REFERENCES[1].O'BrienPM,et,al.Structure-activityrelationshipsandpharmacokineticanalysisforaseriesofpotent,systemicallyavailablebiphenylsulfonamidematrixmetalloproteinaseinhibitors.JMedChem.2000Jan27;43(2):156-66.[2].KaludercicN,et,al.InhibitingmetalloproteaseswithPD166793inheartfailure:impactoncardiacremodelingandbeyond.CardiovascTher.Spring2008;26(1):24-37.[3].ChanceyAL,et,al.Effectsofmatrixmetalloproteinaseinhibitiononventricularremodelingduetovolumeoverload.Circulation.2002Apr23;105(16):1983-8.McePdfHeightMedChemExpress(MCE)只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的?