| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
The mechanism of action of Omberacetam is multifaceted, involving modulation of various neurotransmitter systems within the brain. Studies have shown that it interacts with AMPA receptors, exhibiting competition for the receptor binding sites ([G-³H]Ro 48-8587) in vitro (IC₅₀ = 80 ± 5.6 μM). Additionally, the compound exerts its neuroprotective effects primarily through an antioxidant mechanism, inhibiting the accumulation of intracellular free radicals and lipid peroxidation damage.
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| ln Vitro |
The AMPA receptor ([G-3H]Ro 48-8587) is selectively agonistic for nooglutil, which shows pharmacologically significant competition for the receptor binding site (IC50 = 6.4 +/- 0.2 microM). In contrast, noopept competes for these receptor binding sites, but at a much lower level (IC50 = 80 +/- 5.6 microM) [1]. Following H(2)O(2) treatment, GVS-111 dramatically improves neuronal survival. It has dose-dependent neuroprotective efficacy from 10 nM to 100 microM, with an IC(50) value of 1.21+/-0.07 microM. GVS-111's antioxidant action is demonstrated by its ability to prevent intracellular free radical buildup and lipid peroxidation damage in neurons treated with H(2)O(2) or FeSO(4) [2].
In vitro studies have demonstrated that Omberacetam exhibits significant neuroprotective activity and antioxidant effects. In H₂O₂-treated normal human cortical neurons, GVS-111 increased neuronal survival in a dose-dependent manner from 10 nM to 100 μM, with an IC₅₀ value of 1.21 ± 0.07 μM. The compound inhibited the accumulation of intracellular free radicals and lipid peroxidation damage in neurons treated with H₂O₂ or FeSO₄. Furthermore, in PC12 cells, pretreatment with 10 μM Noopept for 72 hours significantly ameliorated Aβ₂₅₋₃₅-induced cell injury, reducing ROS and intracellular calcium levels, enhancing mitochondrial membrane potential, and attenuating tau hyperphosphorylation. Noopept exhibited significantly higher neuroprotection compared to the standard cognition enhancer Piracetam or antioxidants such as Vitamin E. |
| ln Vivo |
Intravenous administration of N-phenylacetyl-L-prolylglycine ethyl ester (GVS-111) at a dose of 0.5 mg/kg/day was performed initially 1 hour after the ischemic lesion and then 9 days postoperatively. The final dose was given 15 minutes prior to testing, and it attenuated the defect [3]. One hour after a 5-mg/kg intraperitoneal injection, GVS-111 itself was no longer detected in the rat brain, having reached the limit of detection (LOD) under high-performance liquid chromatography (HPLC) conditions [4]. The dipeptide showed the strongest anti-inflammatory effects in a rat model of adjuvant arthritis when it was given at a dose of 0.5 mg/kg (im) or 5 mg/kg (po) every day for 25 days. medication, which on day 12 dramatically decreased the chronic immunological inflammation by 94.0 and 74.1%, respectively [5].
In vivo studies have demonstrated that Omberacetam exhibits neuroprotective, anti-inflammatory, and cognitive-enhancing activities in various animal models. In a rat model of ischemic injury, intravenous administration of GVS-111 (0.5 mg/kg/day for 9 post-operative days) attenuated neurological deficits. In a rat model of adjuvant arthritis, administration of the drug over 25 days (0.5 mg/kg i.m. or 5 mg/kg p.o.) significantly reduced chronic immune inflammation (by 94.0% and 74.1%, respectively, on day 12). In cognitive function studies, Noopept (0.1, 0.5, and 1.0 mg/kg i.p.) eliminated the manifestations of learned helplessness by increasing the percentage of trained animals. |
| Enzyme Assay |
Receptor binding studies of Omberacetam in cell-free systems primarily use radioligand binding assays. The standard protocol includes: 1) Prepare synaptic membranes containing AMPA receptors or cell membranes expressing recombinant receptors; 2) Mix varying concentrations of Noopept (e.g., 0.1-1000 μM) with the selective radiolabeled agonist [G-³H]Ro 48-8587 in binding buffer containing 50 mM Tris-HCl; 3) Incubate at room temperature (25°C) for a period (typically 60 minutes) to reach binding equilibrium; 4) Terminate the reaction by rapid vacuum filtration and measure membrane-bound radioactivity using a liquid scintillation counter; 5) Calculate IC₅₀ values from competition binding curves to evaluate the competitive ability of Noopept at AMPA receptor binding sites (reference value: IC₅₀ = 80 ± 5.6 μM).
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| Cell Assay |
The in vitro cell assay protocol for Omberacetam is as follows: 1) Seed target cells (e.g., human cortical neurons, PC12 cells, or Down's syndrome cortical neurons) in culture plates and culture to appropriate density at 37°C with 5% CO₂; 2) For differentiation experiments, PC12 cells are induced with NGF (50 ng/mL) in DMEM containing 1% FBS for 5 days; 3) Pre-treat cells with various concentrations of Omberacetam (e.g., 10 nM to 100 μM) for 24-72 hours; 4) Expose to injury conditions: such as H₂O₂ (50 μM, 1 hour), FeSO₄, or Aβ₂₅₋₃₅ (5 μM, 24 hours); 5) Assess cell viability using MTT or CCK-8 assays; 6) Measure intracellular ROS levels and calcium concentration using fluorescent probes; 7) Detect apoptosis rate using flow cytometry or TUNEL staining.
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| Animal Protocol |
The in vivo animal assay protocol for Omberacetam is as follows: 1) Use adult male rats or mice to establish disease models, such as ischemic injury model, adjuvant arthritis model, or cognitive impairment model; 2) Randomize animals into model control, vehicle control, positive control, and Omberacetam treatment groups (multiple doses: e.g., 0.1, 0.5, 1.0 mg/kg i.p., or 0.5 mg/kg i.v., or 5 mg/kg p.o.); 3) Dosing regimen: 0.5 mg/kg/day i.v. for 9 days post-surgery in ischemic model; 25 consecutive days in arthritis model; i.p. administration in cognitive studies, typically 30-60 minutes before behavioral testing; 4) Assess cognitive function using behavioral tests (e.g., active avoidance conditioning test); 5) Evaluate inflammatory markers or neurological damage through histopathological analysis; 6) Detect drug concentrations in brain tissue using HPLC.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of Omberacetam indicate that the compound is rapidly metabolized in vivo. One hour after intraperitoneal administration of 5 mg/kg in rats, the parent drug GVS-111 itself was no longer detectable in the brain (reaching below the limit of detection under HPLC conditions). The compound primarily exerts its effects through its metabolites rather than the parent drug directly entering brain tissue. Studies have shown that Noopept eliminates manifestations of learned helplessness by increasing the number of trained animals. It has good oral bioavailability, as demonstrated by significant anti-inflammatory effects at an oral dose of 5 mg/kg in an adjuvant arthritis model, reducing chronic immune inflammation by 74.1% on day 12.
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| Toxicity/Toxicokinetics |
According to the Material Safety Data Sheet, Omberacetam (Noopept) is classified as a non-hazardous substance or mixture, with no GHS hazard classification identified. The toxicological effects have not been thoroughly studied, but according to supplier information, the substance is not classified as a carcinogen by NTP, IARC, OSHA, or ACGIH. In in vitro studies, Omberacetam did not exhibit obvious cytotoxic effects at the tested concentrations. No significant adverse reactions have been reported in animal studies at therapeutic dose ranges. It should be noted that this product is for research use only and is not intended for human or veterinary use.
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| References |
| Molecular Formula |
C17H22N2O4
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|---|---|
| Molecular Weight |
318.373
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| Exact Mass |
318.157
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| Elemental Analysis |
C, 64.13; H, 6.97; N, 8.80; O, 20.10
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| CAS # |
157115-85-0
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| Related CAS # |
157115-85-0;
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| PubChem CID |
180496
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
547.3±50.0 °C at 760 mmHg
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| Melting Point |
94.0 to 98.0 °C
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| Flash Point |
284.8±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.549
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| LogP |
1.28
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
432
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCOC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CC2=CC=CC=C2
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| InChi Key |
PJNSMUBMSNAEEN-AWEZNQCLSA-N
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| InChi Code |
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
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| Chemical Name |
ethyl (2-phenylacetyl)-L-prolylglycinate
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| Synonyms |
DVD-111; GVS-111; SGS-111; Noopept; 157115-85-0; Omberacetam; 4QBJ98683M; DVD111; GVS111; SGS111; DVD 111; GVS 111; SGS 111; Omberacetam
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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 |
| 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 : ≥ 100 mg/mL (~314.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1410 mL | 15.7050 mL | 31.4100 mL | |
| 5 mM | 0.6282 mL | 3.1410 mL | 6.2820 mL | |
| 10 mM | 0.3141 mL | 1.5705 mL | 3.1410 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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