中文名称CS-2890中文同义词化合物BAM15;N5,N6-双(2-氟苯基)-[1,2,5]恶二唑并[3,4-B]吡嗪-5,6-二胺;BAM15,线粒体质子解偶联剂;CS-2890BAM15英文名称BAM15英文同义词BAM15;N,N’-bis(2-fluorophenyl)[1,2,5]oxadiazolo[3,4-b]pyrazine-5,6-diamine;CS-2890;[1,2,5]Oxadiazolo[3,4-b]pyrazine-5,6-diamine,N5,N6-bis(2-fluorophenyl)-;BAM15>=98%(HPLC);BAM15(N5,N6-bis(2-Fluorophenyl)-[1,2,5]oxadiazolo[3,4-b]pyrazine-5,6-diamine);inhibit,BAM-15,Inhibitor,BAM15,BAM15,MitochondrialMetabolismCAS号210302-17-3分子式C16H10F2N6O分子量340.29EINECS号201-118-7相关类别抑制剂Mol文件210302-17-3.mol结构式CS-2890性质沸点421.7±55.0°C(Predicted)密度1.548±0.06g/cm3(Predicted)储存条件-20°C溶解度溶于DMSO(35mg/ml)形态粉末酸度系数(pKa)-2.40±0.50(Predicted)颜色白色至米色稳定性从购买之日起2年内保持稳定。DMSO溶液可在-20°C下保存长达1个月。CS-2890用途与合成方法生物活性BAM15是一种新型的mitochondrialprotonophore的解偶联剂,能够保护哺乳动物免受急性肾缺血-再灌注损伤和冷诱导的微管损伤。BAM15也是一种有效的AMPK激活剂。BAM15可减轻iPS分化的视网膜组织中运输引起的凋亡。靶点TargetValueAMPK()体外研究BAM15isabletoincreaseO2consumptionacrossabroaddosinChemicalbookgrangewithoutincreasingROS.BAM15andFCCParestructurallyunrelatedanditisobservedthatlowdosesofBAM15from100nMto1μMincreasecellularO2consumptionrate(OCR)toasimilardegreeasFCCP,buthigherconcentrationsfrom1μMto50μMrevealthatBAM15isabletomaintainuncoupledrespirationatahighrateinarangeofcelllines.BAM15isfullycapableofincreasingmitochondrialrespirationinthepresenceofoligomycinanddoessoacrossabroaderconcentrationrangethanFCCPinbothmyoblastsandhepatocytes.BAM15inducesmitochondrialswelling,demonstratingthatBAM15isaprotonophore.BAM15-treatedcellsaremoreviablethanFCCP-treatedcellswhenadministeredacrossabroaddosingrangeupto50μM.体内研究Comparetovehicle-treatedmice,animalsthatreceiveBAM15areprotectedfromkidneyinjuryasindicatedbylowerplasmacreatininelevelsat24and48hpost-ischemia,reducedtubularnecrosis,lessdepletionofbrushbordervilli,lessobstructionofproximaltubules,andlessimmunecellinfiltration. |