
戈舍瑞林
Goserelin(ICI 118630)是注射型促性腺激素释放激素(GnRH)超激动剂。
产品名称
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中文名戈舍瑞林
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英文名Goserelin
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中文别名高舍瑞林
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英文别名
(2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-13-(tert-butoxymethyl)-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-10-(4-hydroxybenzyl)-7-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-24-imino-4-(1H-indol-3-ylmethyl)-16-(2-methylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatetracos-1-yl]-5-oxopyrrolidine-2-carboxamide (non-preferred name) 5-Oxo-L-prolyl-L-histidyl-N-[(1S,4S,7R,10S,13S)-18-amino-13-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]-1-pyrrolidinyl}carbonyl)-4-(4-hydroxybenzyl)-1-(hydroxymethyl)-18-imino-10-isobutyl-7-{[(2-methyl-2-propanyl)oxy]methyl}-2,5,8,11-tetraoxo-3,6,9,12,17-pentaazaoctadec-1-yl]-L-tryptophanamide (2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-13-[(1,1-diméthyléthoxy)méthyl]-10-(4-hydroxybenzyl)-7-(hydroxyméthyl)-1-(1H-imidazol- 2-Pyrrolidinecarboxylic acid, 1-[(2S,5S,8R,11S,14S,17S,20S)-2-[3-[(aminoiminomethyl)amino]propyl]-8-[(1,1-dimethylethoxy)methyl]-14-(hydroxymethyl)-11-[(4-hydroxyphenyl)methyl]-20-(1H-imidazol-4-ylmethyl)-17-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-1,4,7,10,13,16,19,22-octaoxo-22-[(2S)-5-oxo-2-pyrrolidinyl]-3,6,9,12,15,18,21-heptaazadocos-1-yl]-, 2-(aminocarbonyl)hydrazide, (2S)- (2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-13-[(1,1-diméthyléthoxy)méthyl]-10-(4-hydroxybenzyl)-7-(hydroxyméthyl)-1-(1H-imidazol-4-ylméthyl)-24-imino-4-(1H-indol-3-ylméthyl)-16-(2-méthylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatétracos-1-yl]-5-oxopyrrolidine-2-carboxamide (2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-13-(tert-butoxymethyl)-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-10-(4-hydroxybenzyl)-7-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-24-imino-4-(1H-indol-3-ylmethyl)-16-(2-methylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatetracos-1-yl]-5-oxopyrrolidine-2-carboxamide Decapeptide I (2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-Amino-13-(tert-butoxymethyl)-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-10-(4-hydroxybenzyl)-7-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-24-imino-4-(1H-indol-3-ylmethyl)-16-(2-methylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatetracos-1-yl]-5-oxopyrrolidin-2-carboxamid 1-(5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-L-prolyl)semicarbazide (2S)-N-[(2S,5S,8S,11S,14R,17S,20S)-25-amino-14-(tert-butoxymethyl)-20-({(2S)-2-[(2-carbamoylhydrazinyl)carbonyl]pyrrolidin-1-yl}carbonyl)-11-(4-hydroxybenzyl)-8-(hydroxymethyl)-1-(1H-imidazol-4-yl)-25-imino-5-(1H-indol-3-ylmethyl)-17-(2-methylpropyl)-3,6,9,12,15,18-hexaoxo-4,7,10,13,16,19,24-heptaazapentacosan-2-yl]-5-oxopyrrolidine-2-carboxamide (non-preferred name) Goserelin (2S)-N-[(2S,5S,8S,11S,14R,17S,20S)-25-Amino-14-(tert-butoxymethyl)-20-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-11-(4-hydroxybenzyl)-8-(hydroxymethyl)-1-(1H-imidazol-4-yl)-25-imino-5-(1H-indol-3-ylmethyl)-17-isobutyl-3,6,9,12,15,18-hexaoxo-4,7,10,13,16,19,24-heptaazapentacosan-2-yl]-5-oxopyrrolidine-2-carboxamide (non-preferred name) -
常用名戈舍瑞林
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C A S号65807-02-5
物理性质
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密度1.5±0.1 g/cm3
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沸点N/A
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熔点N/A
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化学式C59H84N18O14
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结构式
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闪点N/A
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分子量1269.41
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精确质量
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P S A493.39000
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外观形状白色固体
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储存条件−20°C
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稳定性
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水溶解性
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形态
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H L B值
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粘度
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PH值
作用/用途
Goserelin(ICI 118630)是注射型促性腺激素释放激素(GnRH)超激动剂。
制备方法
【方法1】
0.2mmol 5-oxoPro-His-NHNH2悬浮于0.9ml二甲基甲酰胺和0.7ml二甲亚砜的混合溶剂中,在0℃和搅拌下,加入0.8mmol 5.7mol/L盐酸的二氧六环溶液,剧烈搅拌5min,得到澄清的溶液。冷至-20℃,加入0.22mmol亚硝酸叔丁酯,再搅拌25min。冷至-30℃,加入0.8mmol三乙胺来中和。加人冷至-20℃的0.1mmol的L-Trp-Ser-Tyr-D-Ser(t-Bu)-Leu-Arg-PrcrNHNHCONH2二盐酸盐和0.1mmol三乙胺溶于lml二甲基甲酰胺的溶液,然后在4℃下搅拌24h。减压蒸出溶剂,剩余物用Sephadex LH-20进行柱层析,用二甲基甲酰胺洗脱。然后用SephadexG-25来提纯,用正丁醇:乙酸:水:吡啶=5:1:5:1(体积比)来洗脱,可得产物。
0.2mmol 5-oxoPro-His-NHNH2悬浮于0.9ml二甲基甲酰胺和0.7ml二甲亚砜的混合溶剂中,在0℃和搅拌下,加入0.8mmol 5.7mol/L盐酸的二氧六环溶液,剧烈搅拌5min,得到澄清的溶液。冷至-20℃,加入0.22mmol亚硝酸叔丁酯,再搅拌25min。冷至-30℃,加入0.8mmol三乙胺来中和。加人冷至-20℃的0.1mmol的L-Trp-Ser-Tyr-D-Ser(t-Bu)-Leu-Arg-PrcrNHNHCONH2二盐酸盐和0.1mmol三乙胺溶于lml二甲基甲酰胺的溶液,然后在4℃下搅拌24h。减压蒸出溶剂,剩余物用Sephadex LH-20进行柱层析,用二甲基甲酰胺洗脱。然后用SephadexG-25来提纯,用正丁醇:乙酸:水:吡啶=5:1:5:1(体积比)来洗脱,可得产物。
安全提醒
MSDS
原料简介
应用范围
毒性和生态
安全信息
安全声明 (欧洲) | S22-S24/25 |
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WGK德国 | 3 |
是否危险品
危险性
危险类别码
危险等级
触发危险方式
安全技术说明书
环境影响程度
包装与储运
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