| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Gly-Pro-Glu targets the N-methyl-D-aspartate (NMDA) receptor, a ligand-gated ion channel crucial for synaptic plasticity and neuronal communication. It acts as a weak agonist at the glutamate-binding site of the NMDA receptor, inhibiting/disrupting glutamate binding with an IC50 of 14.7 μM. This interaction is dose-dependent and leads to ion channel opening, allowing Ca²⁺ influx. The peptide also modulates acetylcholine release and serves as a substrate for enzymes involved in protein breakdown.
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| ln Vitro |
Even at a dose of 0.1 nM, Gly-Pro-Glu (0-100 μM) increases potassium-induced acetylcholine release and considerably enhances induced dopamine release that is produced by potassium [1]. With an IC50 value of 14.7 μM, Gly-Pro-Glu (1-1000 μM) inhibits the binding of L-[3H]glutamate[1].
In vitro, Gly-Pro-Glu inhibits glutamate binding to NMDA receptors with an IC50 of 14.7 μM. It acts as a weak agonist at the glutamate-binding site of the NMDA receptor, leading to Ca²⁺ influx. The peptide modulates acetylcholine release, influencing cholinergic signaling. These activities suggest a role in neuroprotection and synaptic modulation. It is a neuroactive peptide with potent action on neurotransmitter systems. |
| ln Vivo |
Gly-Pro-Glu (300 mg; intraperitoneally once daily; days 0, 6, and 12) has been demonstrated to provide in vivo protection against Abeta injury to the temporal cortex somatostatinergic system. [2].
In vivo, Gly-Pro-Glu is neuroprotective after central administration in animal models of neurodegenerative processes, including Huntington's, Parkinson's, and Alzheimer's diseases, as well as various acute brain injury models. It protects and rescues cell death induced by amyloid beta-peptide in experimental models. The peptide's neuroprotective effects are attributed to its modulation of NMDA receptor activity and acetylcholine release. |
| Enzyme Assay |
In vitro receptor binding assays for Gly-Pro-Glu typically use membrane preparations from brain tissue or cells expressing NMDA receptors. Radiolabeled glutamate or NMDA receptor ligands (e.g., [³H]MK-801) are used in competition binding experiments. Various concentrations of Gly-Pro-Glu are incubated with membranes and radioligand. Bound radioactivity is measured by scintillation counting. IC50 values are calculated from displacement curves. Functional assays measure calcium flux or electrophysiological responses.
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| Cell Assay |
Cellular assays for Gly-Pro-Glu utilize neuronal cell cultures or brain slices. Cells are treated with Gly-Pro-Glu at various concentrations. NMDA receptor function is assessed by measuring calcium influx using fluorescent calcium indicators (e.g., Fluo-4) following NMDA stimulation. Acetylcholine release is measured in synaptosomal preparations or using microdialysis. Cell viability is assessed in models of excitotoxicity or amyloid-induced toxicity.
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| Animal Protocol |
Animal/Disease Models: Ovariectomized rats were injected with Abeta25-35[2].
Doses: 300 mg. Route of Administration: intraperitoneal (ip) injection; 300 mg per day; results on days 0, 6 and 12: Recovery of Abeta25-35-induced somatostatin (SRIF). ) content and SRIF receptor density were diminished, and the inhibitory effect of SRIF on adenylyl cyclase activity was diminished. In vivo animal studies for Gly-Pro-Glu utilize models of neurodegenerative diseases, such as transgenic mouse models of Alzheimer's disease, MPTP models of Parkinson's disease, or 3-nitropropionic acid models of Huntington's disease. The peptide is administered via intracerebroventricular (ICV) injection or other central routes. Behavioral assessments (memory, motor function) are performed. Neuropathological analysis (amyloid plaque load, neuronal loss, neuroinflammation) is conducted at study termination. |
| ADME/Pharmacokinetics |
Gly-Pro-Glu is a tripeptide with molecular weight of 301.3 g/mol (C₁₂H₁₉N₃O₆). As a peptide, it has limited oral bioavailability and is typically administered via injection or central routes for research purposes. Pharmacokinetic properties include rapid clearance by peptidases. The peptide's short half-life necessitates frequent dosing or continuous administration in vivo studies. It is soluble in water and suitable for in vitro and in vivo research applications.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of Gly-Pro-Glu is not extensively documented. As an endogenous peptide fragment, it is generally considered to have low toxicity. In animal models, central administration of the peptide is well-tolerated. No significant adverse effects have been reported at neuroprotective doses. Standard toxicology studies would be required for therapeutic development. The compound is available for research purposes only.
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| References |
[1]. Sara VR, et al. Identification of Gly-Pro-Glu (GPE), the aminoterminal tripeptide of insulin-like growth factor 1 which is truncated in brain, as a novel neuroactive peptide. Biochem Biophys Res Commun. 1989 Dec 15;165(2):766-71.
[2]. Aguado-Llera D, et al. Gly-Pro-Glu protects beta-amyloid-induced somatostatin depletion in the rat cortex. Neuroreport. 2004 Aug 26;15(12):1979-82. |
| Additional Infomation |
Gly-Pro-Glu is an oligopeptide. Neuren Pharmaceuticals previously developed Glypromate (glycine-proline-glutamate), a natural small-molecule neuroprotective agent derived from IGF-1 that inhibits caspase III-dependent apoptosis, intended for intravenous infusion in the treatment of neurodegenerative diseases. In December 2008, the company discontinued further development of the drug due to its failure to demonstrate observable efficacy.
Drug Indications Investigated for the treatment of neurological disorders. Gly-Pro-Glu (GPE) is the N-terminal tripeptide of IGF-1. It is a neuroactive peptide that modulates NMDA receptor activity (IC50 14.7 μM) and acetylcholine release. It has neuroprotective effects in models of Huntington's, Parkinson's, Alzheimer's, and acute brain injury. It is available for research purposes only. |
| Molecular Formula |
C12H19N3O6
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| Molecular Weight |
301.299
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| Exact Mass |
301.127
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| CAS # |
32302-76-4
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| PubChem CID |
3080768
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| Appearance |
White to off-white solid powder
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| LogP |
-5.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
21
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| Complexity |
439
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(O)CC[C@@H](C(O)=O)NC([C@@H]1CCCN1C(CN)=O)=O
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| InChi Key |
JJGBXTYGTKWGAT-YUMQZZPRSA-N
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| InChi Code |
InChI=1S/C12H19N3O6/c13-6-9(16)15-5-1-2-8(15)11(19)14-7(12(20)21)3-4-10(17)18/h7-8H,1-6,13H2,(H,14,19)(H,17,18)(H,20,21)/t7-,8-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-(2-aminoacetyl)pyrrolidine-2-carbonyl]amino]pentanedioic acid
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| Synonyms |
Glypromate; glycyl-prolyl-glutamic acid; Gly-Pro-Glu
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~221.27 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3190 mL | 16.5948 mL | 33.1895 mL | |
| 5 mM | 0.6638 mL | 3.3190 mL | 6.6379 mL | |
| 10 mM | 0.3319 mL | 1.6595 mL | 3.3190 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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