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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
—— acide mycophenolique 483-60-3 C17H20O6
acide mycophenolique
—— 9-chloro-2-furan-2-yl-6H-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-5-one 104615-00-1 C13H7ClN4O2
9-chloro-2-furan-2-yl-6H-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-5-one
—— GDC-0077 2060571-02-8 C18H19F2N5O4
GDC-0077
—— Cyclopamine 4449-51-8 C27H41NO2
Cyclopamine
—— 17,23-epoxy-veratra-5,12-dien-3-ol 4449-51-8 C27H41NO2
17,23-epoxy-veratra-5,12-dien-3-ol
—— sonidegib 956697-53-3 C26H26F3N3O3
sonidegib
—— sildenafil citrate 171599-83-0 C6H8O7*C22H30N6O4S
sildenafil citrate
—— Tiotropium bromide hydrate 139404-48-1 Br*C19H22NO4S2
Tiotropium bromide hydrate
—— (2S,5R)-N-(2-aminoethoxy)-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide 1452458-86-4 C9H16N4O7S
(2S,5R)-N-(2-aminoethoxy)-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide
—— lomerizine dihydrochloride 101477-54-7 C27H30F2N2O3*2ClH
lomerizine dihydrochloride
—— [(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,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,16E,18R,19R,21R,23S,24E,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
—— Blasticidine S HCl 3513-03-9 C17H27ClN8O5
Blasticidine S HCl
—— D-Phenylalaninamide, N-acetyl-D-tyrosyl-D-arginyl- 1809784-29-9 C26H35N7O5
D-Phenylalaninamide, N-acetyl-D-tyrosyl-D-arginyl-
—— 4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide 1395084-25-9 C18H17N5O3S
4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide
—— pamiparib 1446261-44-4 C16H15FN4O
pamiparib
—— 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine 1800046-95-0 C23H25N9O
6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
—— Piericidin A<sub>1</sub> 2738-64-9 C25H37NO4
Piericidin A<sub>1</sub>
—— piericidin A<sub>1</sub> 2738-64-9 C25H37NO4
piericidin A<sub>1</sub>
—— APG-1387 1570231-89-8 C60H72N10O10S2
APG-1387
—— isopropyl (S)-2-((S)-2-acetamido-3-(1H-indol-3-yl)propanamido)-6-diazo-5-oxohexanoate 2079939-05-0 C22H27N5O5
isopropyl (S)-2-((S)-2-acetamido-3-(1H-indol-3-yl)propanamido)-6-diazo-5-oxohexanoate
—— sodium;2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate;tetrahydrate 201677-61-4 C20H29N2NaO11S
sodium;2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate;tetrahydrate
—— DM4 796073-69-3 C38H54ClN3O10S
DM4
—— Estra-1,3,5(10)-triene-3,17-diol(17b)-, 17-cyclopentanepropanoate 313-06-4 C26H36O3
Estra-1,3,5(10)-triene-3,17-diol(17b)-, 17-cyclopentanepropanoate
—— FSRYAR 725715-18-4 C36H54N12O9
FSRYAR
—— N-(2-(4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl)-1,1-dimethylethyl)methanesulfonamide 642473-62-9 C18H25N5O3S
N-(2-(4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl)-1,1-dimethylethyl)methanesulfonamide
—— Pictilisib dimesylate 957054-33-0 2CH4O3S*C23H27N7O3S2
Pictilisib dimesylate
—— N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline hydrochloride 1352610-25-3 C22H18FN7*ClH
N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline hydrochloride
—— O,O'-Diisobutyroyl-thiamindisulfid 3286-46-2 C32H46N8O6S2
O,O'-Diisobutyroyl-thiamindisulfid
—— benidipine hydrochloride 91599-74-5 C28H31N3O6*ClH
benidipine hydrochloride
—— bromfenac sodium 91714-93-1 C15H11BrNO3*Na
bromfenac sodium
—— 4-(tert-butylsulfonylamino)-N-[5-(trifluoromethyl)pyridin-2-yl]cyclohexane-1-carboxamide 342577-38-2 C17H24F3N3O3S
4-(tert-butylsulfonylamino)-N-[5-(trifluoromethyl)pyridin-2-yl]cyclohexane-1-carboxamide
—— Vodobatinib 1388803-90-4 C27H20ClN3O2
Vodobatinib
—— (1r,4r)-4-((2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl 2-aminoacetate 908115-27-5 C25H30F3N5O4
(1r,4r)-4-((2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl 2-aminoacetate
—— E7016 902128-92-1 C20H19N3O3
E7016
—— cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid 471905-41-6 C21H21ClF2O4S
cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
—— histamine dichloride 56-92-8 C5H11N3*2Cl
histamine dichloride
—— (2E)-3-phenyl-N-[2,2,2-trichloro-1-[[(8-quinolylamino)thiomethyl]amino]ethyl]-2-acrylamide 405060-95-9 C21H17Cl3N4OS
(2E)-3-phenyl-N-[2,2,2-trichloro-1-[[(8-quinolylamino)thiomethyl]amino]ethyl]-2-acrylamide
—— romidepsin 128517-07-7 C24H36N4O6S2
romidepsin
—— [7-[cis-3-[(Azetidin-1-yl)methyl]cyclobutyl]-5-(3-benzyloxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amine 475489-16-8 C27H29N5O
[7-[cis-3-[(Azetidin-1-yl)methyl]cyclobutyl]-5-(3-benzyloxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amine
—— 2-[4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid 1109276-89-2 C21H24N4O4
2-[4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid
—— (+)-Dimethindene 121367-05-3 C20H24N2
(+)-Dimethindene
—— AM211 1175526-27-8 C27H27F3N2O4
AM211
—— Azilsartan medoxomil 863031-21-4 C30H24N4O8
Azilsartan medoxomil
—— Cilomilast 153259-65-5 C20H25NO4
Cilomilast
—— cilomilast 153259-65-5 C20H25NO4
cilomilast
—— 1,1'-[1,4-phenylene-bis(methylene)]-bis(1,4,8,11-tetra-azacyclotetradecane) octahydrochloride 155148-31-5 C28H54N8*8ClH
1,1'-[1,4-phenylene-bis(methylene)]-bis(1,4,8,11-tetra-azacyclotetradecane) octahydrochloride
—— cyclosporin A 59865-13-3 C62H111N11O12
cyclosporin A
—— cyclosporine A 59865-13-3 C62H111N11O12
cyclosporine A
—— (2S,4S,5S,7S)-N-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]octanamide hemifumarate 173334-58-2 C4H4O4*2C30H53N3O6
(2S,4S,5S,7S)-N-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]octanamide hemifumarate
—— 2-(4-(2-(7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-isopropyl-1H-indol-5-yl)piperidin-1-yl)acetamide 2171019-55-7 C26H32N6O
2-(4-(2-(7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-isopropyl-1H-indol-5-yl)piperidin-1-yl)acetamide