N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯

中文名称:

N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯

中文同义词:

苯乙酰甘氨酸乙酯;N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯生产厂家;N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯;N-(1-(苯基乙酰基)-L-脯氨酰) 甘氨酸乙酯 157115-85-0;N-(1-苯基乙酰基)-L-脯氨酰胺甘氨酸乙酯

英文名称:

ethyl 2-[[(2S)-1-(2-phenylacetyl)pyrrolidine-2-carbonyl]amino]acetate

英文同义词:

Noopept;ethyl 2-[[(2S)-1-(2-phenylacetyl)pyrrolidine-2-carbonyl]amino]acetate;N-(1-(Phenylacetyl)-L-prolyl)glycine ethyl ester;Ethyl 1-(phenylacetyl)-L-prolylglycinate;noopept powder;Nootropic GVS-111;(S)-ethyl 2-(1-(2-phenylacetyl)pyrrolidine-2-carboxaMido)acetate;SGS 111

CAS号:

157115-85-0

分子式:

C17H22N2O4

分子量:

318.37

EINECS号:

1592732-453-0

相关类别:

营养剂;化合物;抑制剂;营养品原料;食品添加剂;膜转运/离子通道;医药中间体;pharmaceutical intermediate and medicine grade;原料药API;食品添加;原料;有机中间体

Mol文件:

157115-85-0.mol

熔点 

94.0 to 98.0 °C

沸点 

547.3±50.0 °C(Predicted)

密度 

1.202±0.06 g/cm3(Predicted)

储存条件 

-20°C

形态

powder

酸度系数(pKa)

13.41±0.20(Predicted)

颜色

white to beige

旋光性 (optical activity)

[α]/D -115 to -125°, c = 0.5 in chloroform-d

CAS 数据库

157115-85-0

简介

N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯的商品名NOOPEPT，作为治疗肥胖、酒精依赖性退化或中毒性损伤等疾病。

生物活性

Omberacetam (GVS-111) 是可作为膳食补充剂的多肽。

体外研究

Nooglutil exhibits pharmacologically significant competition with a selective agonist of AMPA receptors ([G-3H]Ro 48-8587) for the receptor binding sites (with IC50 = 6.4 +/- 0.2 microM), while the competition of noopept for these receptor binding sites was lower by an order of magnitude (IC50 = 80 +/- 5.6 microM) [1]. GVS-111 significantly increased neuronal survival after H(2)O(2)-treatment displaying a dose-dependent neuroprotective activity from 10 nM to 100 microM, and an IC(50) value of 1.21+/-0.07 microM. GVS-111 inhibited the accumulation of intracellular free radicals and lipid peroxidation damage in neurons treated with H(2)O(2) or FeSO(4), suggesting an antioxidant mechanism of action [2].

体内研究

N-Phenylacetyl-L-prolylglycine ethyl ester (GVS-111) administered intravenously at a dose of 0.5 mg/kg/day, for the first time 1 h after ischaemic lesion and then for 9 post-operative days, with the last administration 15 min before testing, attenuated the deficit [3]. GVS-111 itself was not found in rat brain 1 h after 5 mg/kg i.p. administration up to limit of detection (LOD) under high performance liquid chromatography (HPLC) conditions [4]. The most pronounced antiinflammatory effect of dipeptide was observed on the model of adjuvant arthritis in rats, where the drug administered over 25 days in a daily dose of 0.5 mg/kg (i.m.) or 5 mg/kg (p.o.) significantly reduced the chronic immune inflammation (on the 12th day, by 94.0 and 74.1%, respectively) [5].

RTECS号

MC0814400

海关编码 

29339900