| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
| Targets |
α-Methyl-DL-aspartic acid targets argininosuccinate synthase (ASS), the rate-limiting enzyme in the conversion of L-citrulline to L-arginine. ASS catalyzes the ATP-dependent condensation of citrulline and aspartate to form argininosuccinate, which is then cleaved to arginine and fumarate. By inhibiting ASS, this compound reduces the intracellular pool of arginine available for nitric oxide synthase (NOS), thereby decreasing NO production. This mechanism has been demonstrated in studies where α-Methyl-DL-aspartic acid diminished the antihypertensive effect of a snake venom peptide (Bj-BPP-10c) in spontaneously hypertensive rats (SHR). The compound's ability to modulate the arginine-NO pathway makes it useful for studying vascular function, blood pressure regulation, and diseases where NO signaling is dysregulated.
|
|---|---|
| ln Vitro |
In SHR, α-Methyl-dl-aspartic acid can greatly diminish Bj-BPP-10c's antihypertensive effect [2].
In vitro, α-Methyl-DL-aspartic acid functions as a specific inhibitor of argininosuccinate synthase (ASS). In spontaneously hypertensive rats (SHR), α-Methyl-DL-aspartic acid can greatly diminish Bj-BPP-10c's antihypertensive effect, confirming its role in modulating the arginine-NO pathway. This suggests that the compound effectively inhibits ASS in biological systems, reducing the availability of arginine for NO production. The compound's inhibitory activity on ASS has been characterized in biochemical assays using purified enzyme or tissue homogenates. By blocking arginine synthesis, the compound serves as a tool for studying the physiological and pathological roles of the urea cycle and arginine metabolism. |
| ln Vivo |
In Wistar rats, the intravenous administration of 147 mg/kg of α-Methyl-dl-aspartate lessens the retinal vasodilation caused by L-citrulline [1].
In vivo, α-Methyl-DL-aspartic acid has been studied in rat models. In Wistar rats, the intravenous administration of 147 mg/kg of α-Methyl-DL-aspartate lessens the retinal vasodilation caused by L-citrulline. This effect is consistent with the compound's mechanism of inhibiting ASS, thereby blocking the conversion of L-citrulline to L-arginine and subsequent NO-mediated vasodilation. This in vivo study demonstrates that the compound is effective at modulating the arginine-NO pathway in a whole-animal context. The compound's ability to attenuate L-citrulline-induced vasodilation highlights its utility for studying the role of the urea cycle and NO signaling in vascular function and diseases such as hypertension and diabetes. |
| Enzyme Assay |
In vitro enzyme assays for argininosuccinate synthase (ASS) inhibition are used to characterize α-Methyl-DL-aspartic acid's activity. ASS catalyzes the conversion of citrulline and aspartate to argininosuccinate in an ATP-dependent reaction. Enzyme activity can be measured by monitoring the production of argininosuccinate or the consumption of ATP using spectrophotometric or HPLC-based methods. The compound is incubated with purified ASS or tissue homogenates at various concentrations, and the IC50 value is determined from dose-response curves. Inhibition of ASS reduces the production of argininosuccinate, which can be quantified to assess the compound's potency. These enzyme assays are essential for characterizing the compound's mechanism of action and potency as an ASS inhibitor.
|
| Cell Assay |
Cell-based assays for α-Methyl-DL-aspartic acid are conducted in relevant cell types such as endothelial cells, macrophages, or cancer cells where arginine metabolism and NO production are important. Cells are treated with the compound at various concentrations, and intracellular arginine levels, NO production (measured by Griess assay or fluorescent NO probes), and downstream signaling are assessed. The compound's effects on cell proliferation, migration, and survival may also be evaluated in the context of arginine-dependent pathways. However, specific detailed cell-based assay protocols for this compound are not extensively documented in the available literature. Researchers should develop appropriate assays based on the compound's mechanism of action and research objectives.
|
| Animal Protocol |
Animal/Disease Models: Wistar rat
Doses: 147 mg/kg Route of Administration: 147 mg/kg, intravenous (iv) (iv)injection Experimental Results: Attenuated the increase in retinal arteriolar diameter caused by L-citrulline. In vivo animal experiments with α-Methyl-DL-aspartic acid have been conducted in Wistar rats. In one study, the compound was administered intravenously at a dose of 147 mg/kg. The experimental endpoint was the measurement of retinal arteriolar diameter to assess the compound's effect on L-citrulline-induced vasodilation. The results showed that α-Methyl-DL-aspartate attenuated the increase in retinal arteriolar diameter caused by L-citrulline. This protocol demonstrates the compound's utility for studying the arginine-NO pathway in vivo. For other research applications, researchers would need to design appropriate animal models and dosing regimens based on the compound's mechanism of action and specific research questions. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of α-Methyl-DL-aspartic acid include its solubility in water (~50 mg/mL, ~339.84 mM). The compound is a white to off-white solid powder with molecular weight 147.13. Specific pharmacokinetic parameters such as half-life, Cmax, AUC, bioavailability, and tissue distribution have not been extensively reported. The compound's small size and high water solubility suggest it may have rapid distribution and clearance, but empirical data are needed for detailed characterization. Storage: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month.
|
| Toxicity/Toxicokinetics |
Toxicology data for α-Methyl-DL-aspartic acid are limited in publicly available sources. The compound is an ASS inhibitor that modulates the arginine-NO pathway, and its pharmacological effects (reduced NO production, altered vascular function) would be the primary considerations for safety. Comprehensive toxicology studies (acute and chronic toxicity, genotoxicity, reproductive toxicity) have not been extensively reported. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. The compound should be stored properly and disposed of in accordance with applicable regulations. Researchers should consult the material safety data sheet (MSDS) for detailed safety information.
|
| References |
|
| Additional Infomation |
α-Methyl-DL-aspartic acid has CAS number 2792-66-7, molecular formula C5H9NO4, and molecular weight 147.13. It is a specific inhibitor of argininosuccinate synthase (ASS), the rate-limiting enzyme for the conversion of L-citrulline to L-arginine. Synonyms: alpha-Methyl-DL-aspartic acid, 2-methylaspartic acid. Purity: ≥98%. Appearance: White to off-white solid powder. Solubility: H2O ~50 mg/mL (~339.84 mM). Storage: powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month. Not approved for clinical use; for research purposes only. The compound is a valuable tool for studying arginine metabolism, the urea cycle, and nitric oxide signaling.
|
| Molecular Formula |
C5H9NO4
|
|---|---|
| Molecular Weight |
147.12926
|
| Exact Mass |
147.053
|
| CAS # |
2792-66-7
|
| PubChem CID |
2109
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
232-234ºC
|
| LogP |
-3.7
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
10
|
| Complexity |
167
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CWAYDJFPMMUKOI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C5H9NO4/c1-5(6,4(9)10)2-3(7)8/h2,6H2,1H3,(H,7,8)(H,9,10)
|
| Chemical Name |
2-amino-2-methylbutanedioic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~50 mg/mL (~339.84 mM)
|
|---|---|
| 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 | 6.7967 mL | 33.9836 mL | 67.9671 mL | |
| 5 mM | 1.3593 mL | 6.7967 mL | 13.5934 mL | |
| 10 mM | 0.6797 mL | 3.3984 mL | 6.7967 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
