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蛋白酶体抑制剂
CAS号 133343-34-7
中文别名
英文别名
分子量 376.42526
分子式 C15H24N2O7S
EINECS编号
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蛋白酶体抑制剂物理化学性质

 熔点 : 233-235°C dec.
储存条件 : −20°C

产品用途

应用领域







化学品安全说明书(MSDS)



储运特性



蛋白酶体抑制剂应用范围 

目前,蛋白酶体抑制剂提取的原材料比较宽泛,如黄豆、青豆、蚕豆、芸豆、豌豆、红小豆、绿豆、花生、 小大麦、玉米、荞麦、麦、香茹、银耳、木耳等。

皮革工业的脱毛和软化已大量利用蛋白酶,既节省时间,又改善劳动卫生条件。蛋白酶还可用于蚕丝脱胶、肉类嫩化、酒类澄清。临床上可作药用,如用胃蛋白酶治疗消化不良,用酸性蛋白酶治疗支气管炎,用惮性蛋白酶治疗脉管炎以及用胰蛋白酶、胰凝乳蛋白酶对外科化脓性创口的净化及胸腔间浆膜粘连的治疗。加酶洗衣粉是洗涤剂中的新产品,含碱性蛋白酶,能去除衣物上的血渍和蛋白污物,但使用时注意不要接触皮肤,以免损伤皮肤表面的蛋白质,引起皮疹、湿疹等过敏现象。

蛋白酶体抑制剂主要来源 

蛋白酶广泛存在于动物内脏、植物茎叶、果实和微生物中。微生物蛋白酶,主要由霉菌、细菌,其次由酵母、放线菌生产。

蛋白酶体抑制剂催化蛋白质水解的酶类。种类很多,重要的有胃蛋白酶、胰蛋白酶、组织蛋白酶、木瓜蛋白酶和枯草杆菌蛋白酶等。蛋白酶对所作用的反应底物有严格的选择性,一种蛋白酶仅能作用于蛋白质分子中一定的肽键,如胰蛋白酶催化水解碱性氨基酸所形成的肽键。蛋白酶分布广,主要存在于人和动物消化道中,在植物和微生物中含量丰富。由于动植物资源有限,工业上生产蛋白酶制剂主要利用枯草杆菌、栖土曲霉等微生物发酵制备。 

蛋白酶体抑制剂酶的定义


 

酶(enzyme)催化特定化学反应的蛋白质、RNA或其复合体。是生物催化剂,能通过降低反应的活化能加快反应速度,但不改变反应的平衡点。绝大多数酶的化学本质是蛋白质。具有催化效率高、专一性强、作用条件温和等特点。酶参与人体所有的生命活动:比如思考,运动,睡眠,呼吸,愤怒,喜悦或者分泌荷尔蒙等都是以酶为中心的活动结果。酶的催化作用催动着机体充满活力的生化反应,催动着生命现象不断健康的运行。同时,国内权威医学证明,酶是人体内新陈代谢的催化剂,只有酶存在,人体内才能进行各项生化反应。人体内酶越多,越完整,其生命就越健康。而都市人普遍存在着缺酶的现象。

蛋白酶体抑制剂重要性

生物体由细胞构成,每个细胞由于酶的存在才表现出种种生命活动,体内的新陈代谢才能进行。酶是人体内新陈代谢的催化剂,只有酶存在,人体内才能进行各项生化反应。人体内酶越多,越完整,其生命就越健康。当人体内没有了活性酶,生命也就结束。人类的疾病,大多数均与酶缺乏或合成障碍有关。

蛋白酶体抑制剂特性 

蛋白酶体抑制剂

1.高效性:酶的催化效率比无机催化剂更高,使得反应速率更快;

2.专一性:一种酶只能催化一种或一类底物,如蛋白酶只能催化蛋白质水解成多肽;因此在食用酵素当今在功能上,主要有四种:高浓缩SOD酵素如复方天然酵素主要用于乳腺瘤、子宫肌瘤、卵巢囊肿等肿瘤方面;长生酵素直接补脾补肾补气血,全面调理;纤体酵素专门转化脂肪减肥;肠毒清酵素则专门清理肠皱褶的毒素。

3.多样性:酶的种类很多,大约有5000多种,其中可以通过食用补充的酵素达2000多种;形态上主要有三种:专业级酵素为酵素胶囊,其次为酵素粉,而液体酵素含量低、效价低、易腐败而安全性较差一些,食用风险较高。

4.温和性:是指酶所催化的化学反应一般是在较温和的条件下进行的,因此,纯正酵素是中性的,温和的,不存在副作用,或“好转反应”。对于有刺激性而必然存的“好转反应”,除了本身腐败以外,也有可能有药品的添加。

5.活性可调节性:包括抑制剂和激活剂调节、反馈抑制调节、共价修饰调节和变构调节等。

6.易变性:大多数酶是蛋白质,因而会被高温、强酸、强碱等破坏;

7.有些酶的催化性与辅助因子有关。

一般来说,动物体内的酶最适温度在35到40℃之间,植物体内的酶最适温度在40-50℃之间;细菌和真菌体内的酶最适温度差别较大,有的酶最适温度可高达70℃。动物体内的酶最适PH大多在6.5-8.0之间,但也有例外,如胃蛋白酶的最适PH为1.8,植物体内的酶最适PH大多在4.5-6.5之间。

酶的这些性质使细胞内错综复杂的物质代谢过程能有条不紊地进行,使物质代谢与正常的生理机能互相适应。若因遗传缺陷造成某个酶缺损,或其它原因造成酶的活性减弱,均可导致该酶催化的反应异常,使物质代谢紊乱,甚至发生疾病,因此酶与医学的关系十分密切。

安全术语
风险术语
上游原料
2-Methylpropanal; Isobutyraldehyde1,3-propanedithiol; 3-sulfanylpropylhydrosulfidemethyl (2R,4S)-3-benzyl-2-(tert-butyl)-1,3-oxazolidine-4-carboxylatemethyl (2R,4R)-3-benzyl-2-(tert-butyl)-4-(1-hydroxy-2-methylpropyl)-1,3-oxazolidine-4-carboxylatemethyl (2R,3S)-2-(benzylamino)-2-([[tert-butyl(dimethyl)silyl]oxy]methyl)-3-hydroxy-4-methylpentanoatemethyl (4R,5S)-3-benzyl-4-([[tert-butyl(dimethyl)silyl]oxy]methyl)-5-isopropyl-1,3-oxazolidine-4-carboxylate(4R,5S)-3-benzyl-4-([[tert-butyl(dimethyl)silyl]oxy]methyl)-5-isopropyl-1,3-oxazolidine-4-carbaldehyde(E)-1-methoxy-1-propenyl trimethylsilyl ether; [[(E)-1-methoxy-1-propenyl]oxy](trimethyl)silanemethyl (2R,3S)-3-[(4S,5S)-3-benzyl-4-([[tert-butyl(dimethyl)silyl]oxy]methyl)-5-isopropyl-1,3-oxazolidin-4-yl]-3-hydroxy-2-methylpropanoate(1S,6R,7S,7aS)-7-hydroxy-7a-(hydroxymethyl)-1-isopropyl-6-methyltetrahydro-5H-pyrrolo[1,2-c][1,3]oxazol-5-one(2R,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxylic acid(1R,4R,5S)-1-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione(2R)-2-(acetamido)-3-sulfanylpropionic acid(E)-4-methyl-2-penten-1-ol[(2R,3S)-3-isopropyloxiranyl]methanol(4R,5S)-3-benzyl-4-(hydroxymethyl)-5-isopropyl-1,3-oxazolidin-2-one(4S,5S)-3-benzyl-5-isopropyl-2-oxo-1,3-oxazolidine-4-carboxylic acidmethyl (4S,5S)-3-benzyl-5-isopropyl-2-oxo-1,3-oxazolidine-4-carboxylate(4R,5S)-3-benzyl-5-isopropyl-2-oxo-1,3-oxazolidine-4-carboxylic acid(2R,3S)-2-amino-3-hydroxy-4-methylpentanoic acidmethyl (2R,3S)-2-amino-3-hydroxy-4-methylpentanoate(4S,5S)-5-isopropyl-4-methyl-2-phenyl-4,5-dihydro-1,3-oxazolemethyl (4S,5S)-4-(hydroxymethyl)-5-isopropyl-2-phenyl-4,5-dihydro-1,3-oxazole-4-carboxylatemethyl (4R,5S)-4-formyl-5-isopropyl-2-phenyl-4,5-dihydro-1,3-oxazole-4-carboxylate(E)-2-butenyl[bis[(1S,2R,3S,5S)-1,2,5,6,6-pentamethylbicyclo[3.1.1]hept-3-yl]]boranemethyl (4S,5S)-4-[(1S,2S)-1-hydroxy-2-methyl-3-butenyl]-5-isopropyl-2-phenyl-4,5-dihydro-1,3-oxazole-4-carboxylate(2R,3S)-3-hydroxy-3-[(4S,5S)-5-isopropyl-4-(methoxycarbonyl)-2-phenyl-4,5-dihydro-1,3-oxazol-4-yl]-2-methylpropionic acid(2S,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxylic acidallyl (2R)-2-(acetamido)-3-sulfanylpropanoateallyl (2R)-2-(acetamido)-3-[([(2S,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxopyrrolidinyl]carbonyl)sulfanyl]propanoate2-Methylpropanal; Isobutyraldehyde(2R,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxylic acid(3S,7aR)-6-methyl-3-phenyl-1,7a-dihydro-5H-pyrrolo[1,2-c][1,3]oxazol-5-one(3S)-5-[[tert-butyl(dimethyl)silyl]oxy]-6-methyl-3-phenyl-1H-pyrrolo[1,2-c][1,3]oxazole; tert-butyl(dimethyl)silyl (3S)-6-methyl-3-phenyl-1H-pyrrolo[1,2-c][1,3]oxazol-5-yl ether(3S,7aR)-7a-[(1S)-1-hydroxy-2-methylpropyl]-6-methyl-3-phenyl-1,7a-dihydro-5H-pyrrolo[1,2-c][1,3]oxazol-5-one(1S)-1-[(3S,6R,7R)-6,7-dihydroxy-6-methyl-5-oxo-3-phenyldihydro-1H-pyrrolo[1,2-c][1,3]oxazol-7(5H)-yl]-2-methylpropyl acetate(1S)-1-[(3S,6S,7S)-7-hydroxy-6-methyl-5-oxo-3-phenyldihydro-1H-pyrrolo[1,2-c][1,3]oxazol-7(5H)-yl]-2-methylpropyl acetate(1S)-1-[(3S,6R,7S)-7-hydroxy-6-methyl-5-oxo-3-phenyldihydro-1H-pyrrolo[1,2-c][1,3]oxazol-7(5H)-yl]-2-methylpropyl acetate(1S)-1-[(2S,3S,4R)-3-hydroxy-2-(hydroxymethyl)-4-methyl-5-oxopyrrolidinyl]-2-methylpropyl acetate(1S)-1-((2R,3S,4R)-3-(acetoxy)-4-methyl-5-oxo-2-[[(triethylsilyl)oxy]methyl]pyrrolidinyl)-2-methylpropyl acetate(1S)-1-[(2R,3S,4R)-3-(acetoxy)-2-(hydroxymethyl)-4-methyl-5-oxopyrrolidinyl]-2-methylpropyl acetate(2R,3S,4R)-3-(acetoxy)-2-[(1S)-1-(acetoxy)-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxylic acid(3S,7aR)-3-phenyltetrahydro-5H-pyrrolo[1,2-c][1,3]oxazol-5-oneethyl 2-(triphenyl-lambda(5)-phosphanylidene)acetate; (Carbethoxymethylene)triphenylphosphorane(1R)-1-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-1,2-ethanediol(1R)-1-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-2-(benzyloxy)-1-ethanol1-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-2-(benzyloxy)-1-ethanoneethyl (E)-3-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-4-(benzyloxy)-2-butenoateethyl (Z)-3-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-4-(benzyloxy)-2-butenoate(Z)-3-[(3aR,5S,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-4-(benzyloxy)-2-buten-1-ol(E)-3-[(3aR,5S,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-4-(benzyloxy)-2-buten-1-ol(Z)-3-[(3aR,5S,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-4-(benzyloxy)-2-butenyl 2,2,2-trichloroethanimidoate(E)-3-[(3aR,5S,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-4-(benzyloxy)-2-butenyl 2,2,2-trichloroethanimidoateN-[(1R)-1-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-1-[(benzyloxy)methyl]-2-propenyl]-2,2,2-trichloroacetamideN-[(1S)-1-[(3aR,6R,6aR)-2,2,6-trimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl]-1-[(benzyloxy)methyl]-2-propenyl]-2,2,2-trichloroacetamideN-[(1R)-1-[(benzyloxy)methyl]-1-[(3S,4R,5S)-4,5-dihydroxy-3-methyltetrahydro-2-furanyl]-2-propenyl]-2,2,2-trichloroacetamide(2R,3S,4R,5R)-2-[(benzyloxy)methyl]-5-hydroxy-4-methyl-1-(2,2,2-trichloroacetyl)-2-vinylpyrrolidinyl formate(2R,3S,4R,5S)-2-[(benzyloxy)methyl]-5-hydroxy-4-methyl-1-(2,2,2-trichloroacetyl)-2-vinylpyrrolidinyl formate(2R,3S,4R)-2-[(benzyloxy)methyl]-4-methyl-5-oxo-1-(2,2,2-trichloroacetyl)-2-vinylpyrrolidinyl formate(3R,4S,5R)-5-[(benzyloxy)methyl]-4-hydroxy-3-methyl-5-vinyl-2-pyrrolidinonebromo(isopropyl)magnesium(2R,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-5-oxo-2-pyrrolidinecarboxylic acid(3R,4S,5R)-5-[(benzyloxy)methyl]-4-hydroxy-3-methyl-5-vinyl-2-pyrrolidinone(3R,4S,5R)-5-[(benzyloxy)methyl]-4-[[tert-butyl(dimethyl)silyl]oxy]-3-methyl-5-vinyl-2-pyrrolidinone(3R,4S,5R)-4-[[tert-butyl(dimethyl)silyl]oxy]-5-(hydroxymethyl)-3-methyl-5-vinyl-2-pyrrolidinone(2S,3S,4R)-3-[[tert-butyl(dimethyl)silyl]oxy]-4-methyl-5-oxo-2-vinyl-2-pyrrolidinecarbaldehyde(3R,4S,5R)-4-[[tert-butyl(dimethyl)silyl]oxy]-5-[(1S)-1-hydroxy-2-methylpropyl]-3-methyl-5-vinyl-2-pyrrolidinone(3R,4S,5R)-4-hydroxy-5-[(1S)-1-hydroxy-2-methylpropyl]-3-methyl-5-vinyl-2-pyrrolidinone(1R,4R,5S)-1-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dionedimethyl 2-methyl-2-(methylsulfanyl)malonate(2S)-3-methoxy-2-methyl-2-(methylsulfanyl)-3-oxopropionic acidmethyl 2-[(4-methoxybenzyl)amino]acetatemethyl (2S,4R)-1-(4-methoxybenzyl)-4-methyl-4-(methylsulfanyl)-3,5-dioxo-2-pyrrolidinecarboxylatemethyl (2R,4R)-1-(4-methoxybenzyl)-4-methyl-4-(methylsulfanyl)-3,5-dioxo-2-pyrrolidinecarboxylatemethyl (2R,3R,4R)-3-hydroxy-2-(hydroxymethyl)-1-(4-methoxybenzyl)-4-methyl-4-(methylsulfanyl)-5-oxo-2-pyrrolidinecarboxylatemethyl (2R,3R,4R)-3-[[tert-butyl(dimethyl)silyl]oxy]-2-(hydroxymethyl)-1-(4-methoxybenzyl)-4-methyl-4-(methylsulfanyl)-5-oxo-2-pyrrolidinecarboxylatemethyl (2S,3S,4R)-3-[[tert-butyl(dimethyl)silyl]oxy]-2-formyl-1-(4-methoxybenzyl)-4-methyl-5-oxo-2-pyrrolidinecarboxylatebromo(isopropenyl)magnesium;isopropenyl magnesium bromide;1-Methylvinylmagnesiumbromide;1-Propen-2-ylmagnesium bromide;a-Methylvinylmagnesium bromidemethyl (2R,3S,4R)-3-[[tert-butyl(dimethyl)silyl]oxy]-2-[(1S)-1-hydroxy-2-methyl-2-propenyl]-1-(4-methoxybenzyl)-4-methyl-5-oxo-2-pyrrolidinecarboxylatemethyl (2R,3S,4R)-3-hydroxy-2-[(1S)-1-hydroxy-2-methylpropyl]-1-(4-methoxybenzyl)-4-methyl-5-oxo-2-pyrrolidinecarboxylate(1R,4R,5S)-1-[(1S)-1-hydroxy-2-methylpropyl]-2-(4-methoxybenzyl)-4-methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dioneEthyl 2-(diethoxyphosphoryl)acetate; Triethyl phosphonoacetate2-Methylpropanal; Isobutyraldehyde(E)-4-methyl-2-penten-1-ol(3S,7aR)-7a-[(1S)-1-hydroxy-2-methylpropyl]-6-methyl-3-phenyl-1,7a-dihydro-5H-pyrrolo[1,2-c][1,3]oxazol-5-one[(2S,3S)-3-isopropyloxiranyl]methanol[(2S,3S)-3-isopropyloxiranyl]methyl 2,2,2-trichloroethanimidoate(1S)-2-methyl-1-[(4R)-2-(trichloromethyl)-4,5-dihydro-1,3-oxazol-4-yl]-1-propanol(4R)-4-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-2-(trichloromethyl)-4,5-dihydro-1,3-oxazole; tert-butyl(dimethyl)silyl (1S)-2-methyl-1-[(4R)-2-(trichloromethyl)-4,5-dihydro-1,3-oxazol-4-yl]propyl ether(2R,3S)-2-amino-3-{[tert-butyl(dimethyl)silyl]oxy}-4-methyl-1-pentanol(5S,6R)-5-isopropyl-2,2,3,3,9,9,10,10-octamethyl-4,8-dioxa-3,9-disilaundecan-6-amine; (1R,2S)-2-{[tert-butyl(dimethyl)silyl]oxy}-1-({[tert-butyl(dimethyl)silyl]oxy}methyl)-3-methylbutylamine(E)-1,3-dibromo-2-methyl-1-propeneN-[(E)-3-bromo-2-methyl-2-propenyl]-N-[(1R,2S)-2-{[tert-butyl(dimethyl)silyl]oxy}-1-({[tert-butyl(dimethyl)silyl]oxy}methyl)-3-methylbutyl]amine; (5S,6R)-N-[(E)-3-bromo-2-methyl-2-propenyl]-5-isopropyl-2,2,3,3,9,9,10,10-octamethyl-4,8-dioxa-3,9-disilaundecan-6-amine(5S,6S)-N-[(Z)-3-bromo-2-methyl-2-propenyl]-5-isopropyl-2,2,3,3,9,9,10,10-octamethyl-4,8-dioxa-3,9-disilaundecan-6-amine; N-[(Z)-3-bromo-2-methyl-2-propenyl]-N-[(1S,2S)-2-{[tert-butyl(dimethyl)silyl]oxy}-1-({[tert-butyl(dimethyl)silyl]oxy}methyl)-3-methylbutyl]amine(2R)-2-({[tert-butyl(dimethyl)silyl]oxy}methyl)-2-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-4-methyl-2,5-dihydro-1H-pyrrole; tert-butyl(dimethyl)silyl (1S)-1-[(2R)-2-({[tert-butyl(dimethyl)silyl]oxy}methyl)-4-methyl-2,5-dihydro-1H-pyrrol-2-yl]-2-methylpropyl ethertert-butyl(dimethyl)silyl (1S)-1-[(2R)-2-({[tert-butyl(dimethyl)silyl]oxy}methyl)-4-methyl-2H-pyrrol-2-yl]-2-methylpropyl ether; (2R)-2-({[tert-butyl(dimethyl)silyl]oxy}methyl)-2-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-4-methyl-2H-pyrrole(5R)-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)-5-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-1-chloro-3-methyl-1,5-dihydro-2H-pyrrol-2-one(5R)-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)-5-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-3-methyl-1,5-dihydro-2H-pyrrol-2-one(5R)-5-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-5-(hydroxymethyl)-3-methyl-1,5-dihydro-2H-pyrrol-2-one(3S,7aS)-7a-((1S)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-methylpropyl)-6-methyl-3-phenyl-1,7a-dihydro-5H-pyrrolo[1,2-c][1,3]oxazol-5-oneethyl (E)-4-methyl-2-pentenoate