| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
| Targets |
Spaglumic Acid functions as a neurotransmitter and a mast cell stabilizer. As the peptide neurotransmitter NAAG, it is a ligand for the metabotropic glutamate receptor 3 (mGluR3) and an inhibitor of NAAG peptidase, which degrades NAAG. As a mast cell stabilizer, it prevents the release of histamine and other inflammatory mediators from mast cells.
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| ln Vitro |
In a dose-dependent manner, β-Spaglumic Acid (63-1000 µM; 2 hours) guards against spinal cord cell damage caused by NMDA [1]. Spinal cord cells are shielded from hypoxia by β-Spaglumic Acid (0-1000 µM; 2 hours) [1]. When neurons are subjected to 25 µM NMDA, intraneuronal free Ca2+ responses are dramatically reduced by 500 µM of β-Spaglumic Acid [1]. In cerebellar granule cells, β-Spaglumic Acid (100 µM; 7 minutes) antagonizes mGluR3 [2].
In vitro, β-Spaglumic Acid (63-1000 µM; 2 hours) guards against spinal cord cell damage caused by NMDA. It also shields spinal cord cells from hypoxia. Its effects are dose-dependent and demonstrate neuroprotective properties, as measured by cell viability and markers of oxidative stress. |
| ln Vivo |
In vivo, Spaglumic Acid is used in patients with allergic conjunctivitis. It is approved in Portugal under the brand name Naabak and in Greece under the brand name Naaxia for use in patients with allergic conjunctivitis. Its mast cell-stabilizing activity contributes to its efficacy in this condition, reducing itching and redness.
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| Enzyme Assay |
In vitro receptor binding assays for Spaglumic Acid typically measure its affinity for the metabotropic glutamate receptor 3 (mGluR3) using radioligand binding techniques. Its ability to inhibit NAAG peptidase can also be assessed using enzymatic assays that measure the degradation of NAAG by the enzyme.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Spinal Cord Cells (NMDA Induced) (Taken from the spinal cord of Sprague-Dawley rat fetuses on prenatal day 15) Tested Concentrations: 63-1000 µM Incubation Duration: 2 hrs (hours) Experimental Results: Results in significant The attenuation concentration of 63 µM can inhibit NMDA toxicity, and the concentrations of 500 and 1000 µM can completely block NMDA toxicity. Clearly, the basal loss of cell viability associated with experimental handling of cells (e.g., serum removal, medium replacement) is minimized. Cell viability assay[1] Cell Types: Spinal Cord Cells (Hypoxia Induced) Tested Concentrations: 0-1000 µM Incubation Duration: 2 hrs (hours) Experimental Results: 8 µM provides 75% protection during hypoxia and completely eliminates hypoxia-induced viability Loss (107.4-114.4% protection at 63-1000 µM, respectively. Cell viability assay [2] Cell Types: Cerebellar Granule Cells (Expressing Group I-III mGluR) Tested Concentrations: 100 µM Incubation Duration: 7 minutes Experimental Results: Passed mGluR3 blockage Inhibition of forskolin- In vitro cellular assays for Spaglumic Acid involve treating neuronal cells or mast cells with the compound and measuring its effects on cell survival (e.g., MTT assay), calcium signaling (using fluorescent dyes), or mediator release (e.g., histamine assay). Its neuroprotective effects against NMDA toxicity and hypoxia have been demonstrated in primary neuronal cultures. |
| Animal Protocol |
In vivo animal models for Spaglumic Acid may include models of allergic conjunctivitis (e.g., ovalbumin-sensitized guinea pigs) or neuroprotective models (e.g., spinal cord injury) to evaluate its mast cell-stabilizing and neuroprotective effects. However, detailed animal protocol information is limited. The compound is used clinically for allergic conjunctivitis.
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| ADME/Pharmacokinetics |
Spaglumic Acid has a molecular formula of C11H16N2O8 and a molecular weight of 304.25 g/mol. Its chemical name is N-acetylaspartylglutamate (NAAG). It is a peptide neurotransmitter and a mast cell stabilizer. The compound is also known as β-NAAG and is approved for use in some countries for allergic conjunctivitis.
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| Toxicity/Toxicokinetics |
Spaglumic Acid is a mast cell stabilizer and neurotransmitter with a well-characterized mechanism of action. It is generally well-tolerated when used as an ophthalmic preparation for allergic conjunctivitis, with minimal systemic absorption. The compound is for research use only and is not approved for human therapeutic use in many regions.
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| References |
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| Additional Infomation |
Spaglumic acid is a peptide.
Spaglumic Acid, also known as N-acetylaspartylglutamate (NAAG) or β-NAAG, is a peptide neurotransmitter and a mast cell stabilizer. It is used in the treatment of allergic conjunctivitis. The compound is for research use only and is not approved for human therapeutic use in many regions. |
| Molecular Formula |
C11H18N2O10
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|---|---|
| Molecular Weight |
338.269
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| Exact Mass |
304.09
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| CAS # |
4910-46-7
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| PubChem CID |
210320
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
769.5±60.0 °C at 760 mmHg
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| Flash Point |
419.1±32.9 °C
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| Vapour Pressure |
0.0±5.7 mmHg at 25°C
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| Index of Refraction |
1.540
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| LogP |
-1.96
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
21
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| Complexity |
448
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(N[C@H](C(O)=O)CC(N[C@H](C(O)=O)CCC(O)=O)=O)=O
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| InChi Key |
GUCKKCMJTSNWCU-BQBZGAKWSA-N
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| InChi Code |
InChI=1S/C11H16N2O8/c1-5(14)12-7(11(20)21)4-8(15)13-6(10(18)19)2-3-9(16)17/h6-7H,2-4H2,1H3,(H,12,14)(H,13,15)(H,16,17)(H,18,19)(H,20,21)/t6-,7-/m0/s1
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| Chemical Name |
(2S)-2-[[(3S)-3-acetamido-3-carboxypropanoyl]amino]pentanedioic acid
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| Synonyms |
Naaxia; Spaglumic Acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.9562 mL | 14.7811 mL | 29.5622 mL | |
| 5 mM | 0.5912 mL | 2.9562 mL | 5.9124 mL | |
| 10 mM | 0.2956 mL | 1.4781 mL | 2.9562 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.
Products are for research use only; We do not sell to patients
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