400-998-5282
专注多肽 服务科研
400-998-5282
专注多肽 服务科研
Glypromate acetate是一种神经保护剂，是一种弱NMDA受体激动剂。
编号：138222
CAS号：32302-76-4
单字母：H2N-GPE-OH
| 编号: | 138222 |
| 中文名称: | Glypromate acetate、IGF-I (1-3) |
| 英文名: | Glypromate acetate、IGF-I (1-3) |
| CAS号: | 32302-76-4 |
| 单字母: | H2N-GPE-OH |
| 三字母: | H2N N端氨基：N-terminal amino group。在肽或多肽链中含有游离a-氨基的氨基酸一端。在表示氨基酸序列时，通常将N端放在肽链的左边。 -Gly甘氨酸：glycine。系统命名为 2-氨基乙酸。是编码氨基酸中没有旋光性的最简单的氨基酸，因具有甜味而得名。符号：G，Gly。 -ProL-脯氨酸：proline。系统命名为吡咯烷-(2S)-羧酸。为亚氨基酸。是编码氨基酸。在肽链中有特殊作用，如易形成顺式的肽键等。符号：P，Pro。 -GluL-谷氨酸：glutamic acid。系统命名为(2S)-氨基-戊二酸。是编码氨基酸。符号：E，Glu。D-谷氨酸存在于多种细菌的细胞壁和某些细菌杆菌肽中。 -OHC端羧基：C-terminal carboxyl group。在肽或多肽链中含有游离羧基的氨基酸一端。在表示氨基酸序列时，通常将C端放在肽链的右边。 |
| 氨基酸个数: | 3 |
| 分子式: | C12H19N3O6 |
| 平均分子量: | 301.3 |
| 精确分子量: | 301.13 |
| 等电点(PI): | 6.36 |
| pH=7.0时的净电荷数: | -0.02 |
| 平均亲水性: | 3 |
| 疏水性值: | -1.83 |
| 外观与性状: | 白色粉末状固体 |
| 消光系数: | - |
| 来源: | 人工化学合成，仅限科学研究使用，不得用于人体。 |
| 纯度: | 95%、98% |
| 盐体系: | 可选TFA、HAc、HCl或其它 |
| 生成周期: | 2-3周 |
| 储存条件: | 负80℃至负20℃ |
| 标签: | 糖尿病(Diabetes) 三肽 |
| 参考文献（References）: | L.Nilsson-Hakansson et al., NeuroReport, 4, 1111 (1993) S.V.Sizonenko et al., Brain Res., 922, 42 (2001) J.Guan et al., Neuropharmacology, 47, 892 (2004) D.Aguado-Llera et al., Neuroreport, 15, 1978 (2004) S.Shapira et al., Neurosci. Lett., 454, 53 (2009) |
这种IGF-I的N-末端三肽促进了乙酰胆碱的体外释放，其效力高出几百倍（10⁻¹⁰ - 10⁻⁶ M） 比完整的IGF-I（4/10⁻⁸ M） ，而缺乏三肽GPE的截短的IGF-I没有显示出任何显著的作用。这增加了GPE可能是IGF-I的活性位点的可能性尽管GPE的确切作用模式尚不清楚，但另一项研究表明，在脑HI损伤后，通过神经胶质细胞局部给予GPE具有神经保护作用。此外，全身给予GPE显示出更广泛的神经保护作用。因此，GPE可能代表IGF-1的中枢和全身抗凋亡作用的互补途径。
This N-terminal tripeptide of IGF-I facilitated the in vitro release of acetylcholine with a several hundredfold higher potency (10⁻¹⁰ - 10⁻⁶ M) than intact IGF-I (4 · 10⁻⁸ M), whereas truncated IGF-I lacking the tripeptide GPE, did not show any significant effect. This raises the possibility that GPE may be the active site of IGF-I. - Although the precise mode of action of GPE is still unknown, another study suggests that local administration of GPE is neuroprotective after brain HI injury via glial cells. In addition, systemic administration of GPE showed a more widespread neuroprotective effect. Therefore, GPE may represent a complementary pathway for central and systemic IGF-1's antiapoptotic effects.
Glypromate acetate是一种神经保护剂，是一种弱NMDA受体激动剂。
Glypromate acetate, a neuroprotective agent, is a weak NMDA receptor agonist.
IGF-I（1-3）H-Gly-Pro-Glu-OH是一种合成肽，已被证明可有效治疗谷氨酸引起的神经元死亡。它与钙离子结合并抑制γ-氨基丁酸的活性，γ-氨基丁酸是一种抑制性神经递质。IGF-I（1-3）H-Gly-Pro-Glu-OH也阻断脂肪酸合成，导致坏死细胞死亡。体外试验表明，该药物可以防止O型红细胞受到磷酸吡哆醛氧化和原儿茶酸结合的影响。这种药物也被证明可以增加小鼠的运动能力，并改善实验性中风大鼠的运动功能。\nIGF-I（1-3）H-Gly-Pro-Glu-OH是使用聚合酶链反应技术合成的，由氨基酸1至3组成
IGF-I (1-3) H-Gly-Pro-Glu-OH is a synthetic peptide that has been shown to be effective in treating neuronal death caused by glutamate. It binds to calcium ions and inhibits the activity of gamma-aminobutyric acid, which is an inhibitory neurotransmitter. IGF-I (1-3) H-Gly-Pro-Glu-OH also blocks fatty acid synthesis, leading to necrotic cell death. In vitro assays have shown that this drug can protect against blood group O erythrocytes from pyridoxal phosphate oxidation and protocatechuic acid binding. This drug has also been shown to increase locomotor activity in mice, as well as improve motor function in rats with experimental stroke.\nIGF-I (1-3) H-Gly-Pro-Glu-OH is synthesized using a polymerase chain reaction technique and consists of amino acids 1 through 3 of
| DOI | 名称 | |
|---|---|---|
| 10.1016/s0006-8993(01)03148-1 | Neuroprotective effects of the N-terminal tripeptide of IGF-1, glycine-proline-glutamate, in the immature rat brain after hypoxic-ischemic injury | 下载 |
| 10.1093/brain/awh156 | Simultaneous neuroprotection and blockade of inflammation reverses autoimmune encephalomyelitis | 下载 |
| 10.1097/01.wnr.0000127461.15985.07 | N-terminal tripeptide of IGF-1 improves functional deficits after 6-OHDA lesion in rats | 下载 |
| 10.1016/j.neuropharm.2004.07.002 | Neuroprotective effects of the N-terminal tripeptide of insulin-like growth factor-1, glycine-proline-glutamate (GPE) following intravenous infusion in hypoxic-ischemic adult rats | 下载 |
| 10.1111/j.1471-4159.2009.05980.x | The N-terminal tripeptide of insulin-like growth factor-I protects against beta-amyloid-induced somatostatin depletion by calcium and glycogen synthase kinase 3 beta modulation | 下载 |
| 10.1016/j.neulet.2009.03.003 | Delayed peripheral administration of the N-terminal tripeptide of IGF-1 (GPE) reduces brain damage following microsphere induced embolic damage in young adult and aged rats | 下载 |
| 10.2174/138955712798868995 | GPE and GPE analogues as promising neuroprotective agents | 下载 |
| 10.1016/j.neuron.2013.07.023 | Environmental enrichment rescues binocular matching of orientation preference in mice that have a precocious critical period | 下载 |
