N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯

简介生物活性体外研究体内研究 N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯试剂级价格

CAS号:157115-85-0
英文名:Noopept
中文名:N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯
CBNumber:CB21876372
分子式:C17H22N2O4
分子量:318.37
MOL File:157115-85-0.mol

N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯化学性质

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
溶解度 :Soluble in DMSO (up to 25 mg/ml)
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
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
InChI :InChI=1S/C17H22N2O4/c1-2-23-16(21)12-18-17(22)14-9-6-10-19(14)15(20)11-13-7-4-3-5-8-13/h3-5,7-8,14H,2,6,9-12H2,1H3,(H,18,22)/t14-/m0/s1
InChIKey :PJNSMUBMSNAEEN-AWEZNQCLSA-N
SMILES :C(OCC)(=O)CNC(=O)[C@@H]1CCCN1C(CC1=CC=CC=C1)=O
CAS 数据库 :157115-85-0

安全信息

RTECS号 :MC0814400
海关编码 :29339900

N-(1-(苯基乙酰基)-L-脯氨酰)甘氨酸乙酯性质、用途与生产工艺

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].