多佐胺

中文名称多佐胺中文同义词多佐胺杂质;多佐胺/杜塞酰胺;(2R,4R)-2-乙基氨基-4-甲基-5,5-二氧代-5,7-二硫杂双环[4.3.0]壬-8,10-二烯-8-磺酰胺;多佐胺-2-6;杜塞酰胺;多佐胺;多佐胺盐酸盐;蒲勒酮英文名称Dorzolamide英文同义词DORZOLAMIDE;DORZOLAMIDE(SUBJECTTOPATENTFREE);4H-Thieno[2,3-b]thiopyran-2-sulfonamide,4-(ethylamino)-5,6-dihydro-6-methyl-,7,7-dioxide,(4S,6S)-;4H-Thieno[2,3-b]thiopyran-2-sulfonamide,4-(ethylamino)-5,6-dihydro-6-methyl-,7,7-dioxide,(4S-trans)-;4S,6S-Dorzolamide;(4S,6S)-4H-Thieno[2,3-b]thiopyran-2-sulfonamide,4-(ethylamino)-5,6-dihydro-6-methyl-,7,7-dioxide;(4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-7,;DorzalamidehydrochlorideCAS号120279-96-1分子式C10H16N2O4S3分子量324.44EINECS号1533716-785-6相关类别Mol文件120279-96-1.mol结构式多佐胺性质沸点575.8±60.0°C(Predicted)密度1.53±0.1g/cm3(Predicted)储存条件roomtemp溶解度DMSO：可溶5mg/mL（透明溶液，加热）酸度系数(pKa)pKa6.35(Uncertain);8.50(Uncertain)形态粉末颜色白色至米色旋光度(OpticalRotation)[α]/D-25to-35°,c=1inmethanolCAS数据库120279-96-1(CASDataBaseReference)多佐胺用途与合成方法生物活性Dorzolamide(L671152)是有效的碳酸酐酶carbonicanhydraseII的抑制剂，其对红细胞CA-II和CA-I的IC50值分别为0.18nM和600nM。体外研究ComponentA,causedbyaninwardfluxofCO2anditssubsequenthydrationbyCA-II,isblockedbyDorzolamideinadose-dependentmannerwithan50%inhibitoryconcentrationIC50of2.4μM(95%confidenceinterval:0.5-10.85μM).体内研究Dorzolamide(3,10,or30mg/kg/day,ip)synergizedmitomycinCexhibitsanti-tumoractivityinEACsolidtumormodels.Dorzolamideproducesadose-dependentdecreaseinthecalculatedratio(relativevalueof57.3±1,25.5±1.8,and24.3±0.7%,respectively).AnimalModel:FemaleSwissalbinomice(EACsolidtumor).Dosage:3,10,or30mg/kg/day(synergizedmitomycinC).Administration:IP,dailyfor3weeks.Result:UpregulatedTXNIPandp53whiledownregulatedbcl-2.EffectiveinretardingthegrowthofEACinmice.