Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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5g |
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Other Sizes |
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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].
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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].
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References |
[1]. Firstova IuIu, et al. Studying specific effects of nootropic drugs on glutamate receptors in the rat brain. Eksp Klin Farmakol. 2011;74(1):6-10.
[2]. Pelsman A, et al. GVS-111 prevents oxidative damage and apoptosis in normal and Down's syndrome human cortical neurons. Int J Dev Neurosci. 2003 May;21(3):117-24. [3]. Ostrovskaya RU, et al. Memory restoring and neuroprotective effects of the proline-containing dipeptide, GVS-111, in a photochemical stroke model. Behav Pharmacol. 1999 Sep;10(5):549-53. [4]. Gudasheva TA, et al. The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine. Eur J Drug Metab Pharmacokinet. 1997 Jul-Sep;22(3):245-52. [5]. Kovalenko LP, et al. Anti-inflammatory properties of noopept (dipeptide nootropic agent GVS-111). Eksp Klin Farmakol. 2002 Mar-Apr;65(2):53-5. [6]. Kovalenko LP, et al. Preclinical study of noopept toxicity. Eksp Klin Farmakol. 2002 Jan-Feb;65(1):62-4. |
Molecular Formula |
C17H22N2O4
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Molecular Weight |
318.373
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Exact Mass |
318.158
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CAS # |
157115-85-0
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Related CAS # |
157115-85-0;
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(OCC)CNC([C@H]1N(C(CC2=CC=CC=C2)=O)CCC1)=O
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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 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.