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抑制剂

抑制剂简介

抑制剂是一类能够降低或阻止生物体内的酶活性、受体的活性或是细胞内特定反应过程的小分子化合物。它们在有机化学、化学化工和生物医药领域中有着广泛的应用,尤其是在药物研发方面。

分类与作用机制

  1. 竞争性抑制剂:这类抑制剂通过与其目标蛋白质(如酶)结合,占据其底物结合位点,从而阻止真正的底物与蛋白质的正常结合。这种类型的抑制通常可以通过增加底物浓度来缓解。
  2. 非竞争性抑制剂:非竞争性抑制剂通过改变蛋白质的功能状态或结构,而不直接与其活性部位相结合。它们可能会影响蛋白质的构象变化或者与其他位点相互作用。
  3. 不可逆抑制剂:这类抑制剂与酶或其他生物分子形成共价键,导致其永久失去功能。由于这种特性,此类抑制剂通常用于实验室研究中。

应用领域

  1. 药物开发:在生物医药领域,抑制剂被广泛用作潜在的治疗药物,用于对抗各种疾病如癌症、病毒感染等。
  2. 酶学研究:有机化学和生物化学研究经常使用特定类型的抑制剂来探究酶的功能和作用机理。
  3. 合成与催化:化学化工中,通过调节反应条件或引入适当的抑制剂可以提高某些目标产物的选择性。

总结

抑制剂的研究和发展对于理解生命过程至关重要,并在药物开发、基础科学研究等多个领域发挥着重要作用。随着技术的进步,新的抑制剂不断被发现和开发出来,为医学治疗提供了更多的可能性。

中文名称 英文名称 CAS号 化学式 结构式图片
—— [(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16Z,18R,19R,21R,23S,24Z,26Z,28Z,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate 162635-04-3 C56H87NO16
[(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16Z,18R,19R,21R,23S,24Z,26Z,28Z,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
—— (1R,9S,12S,15R,16E,18R,21R,23S,24E,26E,28E,30S,32S,35R)-12-[(2R)-1-[(1S,3R,4R)-4-dimethylphosphoryloxy-3-methoxycyclohexyl]propan-2-yl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone 572924-54-0 C53H84NO14P
(1R,9S,12S,15R,16E,18R,21R,23S,24E,26E,28E,30S,32S,35R)-12-[(2R)-1-[(1S,3R,4R)-4-dimethylphosphoryloxy-3-methoxycyclohexyl]propan-2-yl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
—— festinavir 634907-30-5 C12H12N2O4
festinavir
—— Scopine 498-45-3 C8H13NO2
Scopine
—— 9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicacid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, (9S,10R,12R)- 99570-78-2 C26H19N3O5
9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicacid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, (9S,10R,12R)-
—— tiotropium bromide 139404-48-1 Br*C19H22NO4S2
tiotropium bromide
—— 2-amino-3-benzoylbenzeneacetic acid sodium salt monohydrate 61618-27-7 C15H12NO3*H2O*Na
2-amino-3-benzoylbenzeneacetic acid sodium salt monohydrate
—— ranolazine dihydrochloride 95635-56-6 C24H33N3O4*2ClH
ranolazine dihydrochloride
—— [4-[2-(1H-indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone 1000669-72-6 C20H20N4O
[4-[2-(1H-indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone
—— androst-3α-hydroxy-5α-hydro-17-one 53-41-8 C19H30O2
androst-3α-hydroxy-5α-hydro-17-one
—— 3β-hydroxy-(5α)-androstan-17-one 53-41-8 C19H30O2
3β-hydroxy-(5α)-androstan-17-one
—— etiocholanolone 53-41-8 C19H30O2
etiocholanolone
—— epiandrosterone 53-41-8 C19H30O2
epiandrosterone
—— androst-3α-hydroxy-5β-hydro-17-one 53-41-8 C19H30O2
androst-3α-hydroxy-5β-hydro-17-one
—— androsterone 53-41-8 C19H30O2
androsterone
—— <i>rac</i>-3β-hydroxy-(5α,13α)-androstan-17-one 53-41-8 C19H30O2
<i>rac</i>-3β-hydroxy-(5α,13α)-androstan-17-one
—— 3β-hydroxy-(5ξ)-androstan-17-one 53-41-8 C19H30O2
3β-hydroxy-(5ξ)-androstan-17-one
—— 3β-hydroxy-(5β)-androstan-17-one 53-41-8 C19H30O2
3β-hydroxy-(5β)-androstan-17-one
—— EUK-134 81065-76-1 C18H18ClMnN2O4
EUK-134
—— 2-[5-(3,5-dimethylpyrazol-1-yl)pentylthio]-4,5-diphenyl imidazole 136609-26-2 C25H28N4S
2-[5-(3,5-dimethylpyrazol-1-yl)pentylthio]-4,5-diphenyl imidazole
—— (S)-3-{4-[5-(2-cyclopentyl-6-methoxypyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methylphenoxy}propane-1,2-diol 1262414-04-9 C25H31N3O5
(S)-3-{4-[5-(2-cyclopentyl-6-methoxypyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methylphenoxy}propane-1,2-diol
—— 5-(5-methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy) phenyl)-1,2,4-oxadiazole 1570496-34-2 C25H25F3N6O4S
5-(5-methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy) phenyl)-1,2,4-oxadiazole
—— M2698 1379545-95-5 C21H19ClF3N5O
M2698
—— flupirtine maleate 75507-68-5 C4H4O4*C15H17FN4O2
flupirtine maleate
—— 2-[2-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-3-isoquinolinecarboxylic acid, hydrochloride 82586-52-5 C27H34N2O7*ClH
2-[2-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-3-isoquinolinecarboxylic acid, hydrochloride
—— dolutegravir sodium 1051375-19-9 C20H18F2N3O5*Na
dolutegravir sodium
—— 9-[4-(cyclohexyloxy)phenyl]-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide 1358751-06-0 C19H23N3O3S
9-[4-(cyclohexyloxy)phenyl]-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide
—— sinefungin 58944-73-3 C15H23N7O5
sinefungin
—— 4-(((3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-((R)-2-((4-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-octadecahydro-2H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid 1443460-91-0 C48H73ClN2O6
4-(((3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-((R)-2-((4-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-octadecahydro-2H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid
—— pregna-4,6-diene-3,20-dione 152-62-5 C21H28O2
pregna-4,6-diene-3,20-dione
—— Buclizin-hydrochlorid 129-74-8 C28H33ClN2*ClH
Buclizin-hydrochlorid
—— phenserine 159652-53-6 C20H23N3O2
phenserine
—— teriflunomide 108605-62-5 C12H9F3N2O2
teriflunomide
—— [(7-hydroxy-5-phenethyl[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)amino]acetic acid 1262132-81-9 C17H16N4O4
[(7-hydroxy-5-phenethyl[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)amino]acetic acid
—— (S)-5-(5-chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one 1448867-41-1 C26H24Cl2N6O4
(S)-5-(5-chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one
—— enalaprilic acid 84680-54-6 C18H24N2O5*2H2O
enalaprilic acid
—— 4-(2-(4-tolylsulfanyl)phenyl)piperidin hydrobromide 960151-65-9 BrH*C18H21NS
4-(2-(4-tolylsulfanyl)phenyl)piperidin hydrobromide
—— MKC-8866 1338934-59-0 C18H19NO7
MKC-8866
—— (+/-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine 70449-94-4 C16H15N
(+/-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine
—— FK506 104987-11-3 C44H69NO12
FK506
—— 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione 1401682-78-7 C24H20F2N6O3
5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione
—— 6α,11β,16α-6,9-difluoro-11,17,21-trihydroxy-16α-methyl-pregna-1,4-diene-3,20-dione 2135-17-3 C22H28F2O5
6α,11β,16α-6,9-difluoro-11,17,21-trihydroxy-16α-methyl-pregna-1,4-diene-3,20-dione
—— 3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol 867160-71-2 C26H23N5O
3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol
—— 3-hydroxy-5α-androstane-17-one 481-29-8 C19H30O2
3-hydroxy-5α-androstane-17-one
—— 5-quinoxalin-6-methylene-1,3-thiazolidine-2,4-dione 648450-29-7 C12H7N3O2S
5-quinoxalin-6-methylene-1,3-thiazolidine-2,4-dione
—— asenapine maleate 85650-56-2 C4H4O4*C17H16ClNO
asenapine maleate
—— 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoate sodium salt 1028486-06-7 C27H19ClFN4O4*Na
4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoate sodium salt
—— AZD1979 1254035-84-1 C25H26N4O5
AZD1979
—— (2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4(dimethylamino)-2-butenamide dimaleate 850140-73-7 C4H4O4*C24H25ClFN5O3
(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4(dimethylamino)-2-butenamide dimaleate
—— 4-Hydroxy-androst-4-en-3,17-dion 566-48-3 C19H26O3
4-Hydroxy-androst-4-en-3,17-dion