| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
Nitric oxide synthase (NOS), specifically all three isoforms: endothelial NOS (eNOS), neuronal NOS (nNOS), and inducible NOS (iNOS). Asymmetric dimethylarginine acts as an endogenous competitive inhibitor of NOS, competing with L-arginine for the enzyme's active site. By inhibiting NOS, ADMA reduces the production of nitric oxide (NO), a critical vasodilator and regulator of vascular homeostasis. Elevated levels of ADMA are associated with impaired endothelial function and are considered a biomarker for cardiovascular disease risk.
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| ln Vitro |
Asymmetric dimethylarginine dihydrochloride is a potent endogenous inhibitor of nitric oxide synthase. It competitively inhibits NOS activity, leading to reduced NO production. In vitro studies have demonstrated that ADMA attenuates endothelium-dependent vasodilation by reducing NO bioavailability. The compound's inhibitory effect on NOS is dose-dependent, and it has been shown to impair endothelial function in various in vitro models using cultured endothelial cells and isolated blood vessels.
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| ln Vivo |
In vivo, elevated levels of asymmetric dimethylarginine are associated with endothelial dysfunction and cardiovascular disease. Administration of ADMA in animal models has been shown to increase blood pressure, reduce renal blood flow, and impair vascular reactivity. The compound is used as a tool to study the pathophysiology of endothelial dysfunction and to evaluate the effects of NOS inhibition on cardiovascular and renal function in vivo.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for asymmetric dimethylarginine dihydrochloride typically involves measuring the inhibition of purified NOS enzyme activity. The assay is performed by incubating recombinant or purified NOS (eNOS, nNOS, or iNOS) with L-arginine substrate and essential cofactors (NADPH, BH4, FAD, FMN) in the presence of varying concentrations of ADMA. The production of nitric oxide (measured as nitrite using the Griess reagent) or the conversion of L-arginine to L-citrulline is quantified. The inhibition constant (Ki) is calculated from dose-response curves.
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| Cell Assay |
In vitro cellular assays for asymmetric dimethylarginine dihydrochloride are performed using cultured endothelial cells (e.g., human umbilical vein endothelial cells, HUVECs) or other NOS-expressing cell lines. Cells are treated with varying concentrations of ADMA, and NOS activity is assessed by measuring NO production using fluorescent probes such as DAF-FM DA or by quantifying nitrite/nitrate accumulation in the culture medium using the Griess assay. Endothelial function is evaluated by assessing the expression of adhesion molecules, endothelial permeability, or the phosphorylation status of eNOS.
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| Animal Protocol |
In vivo animal experiments for asymmetric dimethylarginine dihydrochloride are conducted in rodent models (rats or mice). ADMA is administered via intravenous injection, intraperitoneal injection, or osmotic minipumps for continuous infusion. Blood pressure is measured using telemetry or tail-cuff methods. Renal blood flow and glomerular filtration rate are assessed using clearance techniques. Vascular reactivity is evaluated in isolated aortic rings or by measuring flow-mediated dilation. Endothelial dysfunction biomarkers, including plasma ADMA levels and NO metabolites, are quantified.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for asymmetric dimethylarginine dihydrochloride are derived from endogenous ADMA metabolism studies. ADMA is primarily eliminated by hydrolysis via dimethylarginine dimethylaminohydrolase (DDAH) to citrulline and dimethylamine, with a small fraction excreted renally. The plasma half-life of ADMA in humans is approximately 3-4 hours. The compound is a naturally occurring metabolite and its levels are regulated by DDAH activity and renal function.
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| Toxicity/Toxicokinetics |
As an endogenous compound, asymmetric dimethylarginine is present in human plasma at concentrations of approximately 0.5-1.0 μM. Elevated ADMA levels are associated with cardiovascular risk factors and diseases, including hypertension, atherosclerosis, and chronic kidney disease. The compound's toxicity is primarily related to its pathophysiological effects on endothelial function rather than direct cytotoxicity.
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| References | |
| Additional Infomation |
Asymmetric dimethylarginine dihydrochloride (CAS: 220805-22-1) has a molecular formula of C8H20Cl2N4O2 and a molecular weight of 275.18. It is also known as NG,NG-Dimethylarginine dihydrochloride. ADMA is an endogenous NOS inhibitor and a well-established biomarker for endothelial dysfunction and cardiovascular risk. The compound is widely used in cardiovascular research to study the role of NO in vascular homeostasis and disease. It is not approved for human use and is intended for research purposes only.
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| Molecular Formula |
C8H18N4O2.2[HCL]
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|---|---|
| Molecular Weight |
275.176
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| Exact Mass |
274.096
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| CAS # |
220805-22-1
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| Related CAS # |
Asymmetric dimethylarginine;30315-93-6;Asymmetric-dimethylarginine-d6 dihydrochloride;1313730-20-9
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| PubChem CID |
16219246
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
427.5ºC at 760 mmHg
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| Melting Point |
202-204OºC
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| Flash Point |
212.4ºC
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| Vapour Pressure |
1.66E-08mmHg at 25°C
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| LogP |
2.059
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
16
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| Complexity |
215
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN(C)C(=N)NCCC[C@@H](C(=O)O)N.Cl.Cl
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| InChi Key |
SYLNVYJOPZWPJI-ILKKLZGPSA-N
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| InChi Code |
InChI=1S/C8H18N4O2.2ClH/c1-12(2)8(10)11-5-3-4-6(9)7(13)14;;/h6H,3-5,9H2,1-2H3,(H2,10,11)(H,13,14);2*1H/t6-;;/m0../s1
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| Chemical Name |
(2S)-2-amino-5-[[amino(dimethylamino)methylidene]amino]pentanoic acid;dihydrochloride
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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 | 3.6340 mL | 18.1699 mL | 36.3399 mL | |
| 5 mM | 0.7268 mL | 3.6340 mL | 7.2680 mL | |
| 10 mM | 0.3634 mL | 1.8170 mL | 3.6340 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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