| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
nNOS 0.3 μM (Ki); iNOS 3 μM (Ki); eNOS 2.5 μM (Ki)
NG-Amino-L-arginine targets the enzyme nitric oxide synthase (NOS). It inhibits all three NOS isoforms: nNOS, iNOS, and eNOS. These enzymes catalyze the conversion of L-arginine to L-citrulline and the signaling molecule nitric oxide (NO). NG-Amino-L-arginine is a reversible NOS inhibitor, distinguishing it from the more commonly used irreversible inhibitor, L-NAME. It acts as a competitive inhibitor at the L-arginine binding site. |
|---|---|
| ln Vitro |
NG-Amino-L-arginine hydrochloride induces inactivation of the citrulline-forming activity of the nNOS, iNOS, and eNOS isoforms with Ki values of 0.3 microM, 3 microM, and 2.5 microM, respectively. This demonstrates its potent inhibitory activity against all three NOS isoforms, with the strongest effect on nNOS. As a reversible inhibitor, it is an excellent tool for studying NOS-dependent processes without the permanent enzyme modification caused by L-NAME.
|
| ln Vivo |
No specific in vivo data was found for NG-Amino-L-arginine hydrochloride. As a potent NOS inhibitor, it will effectively block the production of nitric oxide in vivo. This inhibition would be expected to have wide-ranging effects, such as increasing blood pressure (by blocking eNOS in vasculature), modulating neuroinflammation (by blocking nNOS and iNOS in the brain), and suppressing inflammatory responses (by blocking iNOS in immune cells).
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| Enzyme Assay |
Standard NOS enzyme activity assay: The citrulline-forming activity of NOS is measured. The reaction mixture contains a NOS isoform (nNOS, iNOS, or eNOS), L-arginine, and other cofactors (NADPH, Ca2+, calmodulin, BH4). NG-Amino-L-arginine hydrochloride is added at varying concentrations, and the reaction is allowed to proceed for a set time. The production of [3H]L-citrulline is measured to calculate the percent inhibition. The Ki value is determined from a Lineweaver-Burk plot.
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| Cell Assay |
Standard cell-based NO production assay: Macrophage cell lines (e.g., RAW 264.7) can be stimulated with LPS to upregulate iNOS activity. The cells are pre-incubated with varying concentrations of NG-Amino-L-arginine hydrochloride. The amount of nitric oxide produced is measured indirectly by quantifying the accumulation of its stable breakdown product, nitrite (NO2-), in the culture supernatant using the Griess reagent assay. The IC50 for inhibition of nitrite production is calculated.
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| Animal Protocol |
No specific animal protocol was found. A typical in vivo protocol to test NOS inhibition: Male Sprague-Dawley rats are anesthetized, and a catheter is placed in the carotid artery to measure mean arterial pressure (MAP). NG-Amino-L-arginine hydrochloride is administered intravenously (e.g., at a dose range of 1-10 mg/kg). The change in MAP is recorded over time. The effect of the compound could be compared to that of a standard NOS inhibitor like L-NAME.
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| ADME/Pharmacokinetics |
No specific PK data was found. NG-Amino-L-arginine hydrochloride is a small, positively charged amino acid analog. Like other NOS inhibitors, it is expected to be rapidly cleared by the kidneys. Its half-life is likely to be short (minutes) due to renal excretion and potential metabolism. It is expected to be distributed to tissues that express NOS enzymes.
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| Toxicity/Toxicokinetics |
No specific toxicity data was found. As a potent NOS inhibitor, NG-Amino-L-arginine could cause significant on-target toxicities, such as hypertension, thrombosis, and tissue damage, due to the suppression of endothelial NO production. It should be handled with caution. The most common NOS inhibitors have been shown to cause fetal harm, are not for human use.
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| References | |
| Additional Infomation |
NG-Amino-L-arginine hydrochloride (CAS: 1031799-40-2) has a molecular formula of C6H15N5O2.HCl and a molecular weight of 225.68. It is an L-arginine analog and a reversible NOS inhibitor with Ki values of 0.3 uM (nNOS), 3 uM (iNOS), and 2.5 uM (eNOS). It is for research use only.
|
| Molecular Formula |
C6H16CLN5O2
|
|---|---|
| Molecular Weight |
225.68
|
| Exact Mass |
225.099
|
| CAS # |
1031799-40-2
|
| PubChem CID |
91886146
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| Appearance |
Typically exists as solids at room temperature
|
| LogP |
1.25
|
| Hydrogen Bond Donor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
14
|
| Complexity |
193
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(C[C@@H](C(=O)O)N)CNC(=N)NN.Cl
|
| InChi Key |
YGVMJVSXFJRHGQ-WCCKRBBISA-N
|
| InChi Code |
InChI=1S/C6H15N5O2.ClH/c7-4(5(12)13)2-1-3-10-6(8)11-9;/h4H,1-3,7,9H2,(H,12,13)(H3,8,10,11);1H/t4-;/m0./s1
|
| Chemical Name |
(2S)-2-amino-5-[[amino(hydrazinyl)methylidene]amino]pentanoic acid;hydrochloride
|
| 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 | 4.4311 mL | 22.1553 mL | 44.3105 mL | |
| 5 mM | 0.8862 mL | 4.4311 mL | 8.8621 mL | |
| 10 mM | 0.4431 mL | 2.2155 mL | 4.4311 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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