Agmatine is a primary amino compound belonging to the Agmatine family. It is a metabolite of E. coli and mice and is the conjugate base of the Agmatine ion (2+). Agmatine is a natural metabolite of the amino acid arginine. It is produced by the decarboxylation of arginine catalyzed by arginine decarboxylase and is naturally found in ragweed pollen, ergot, octopus muscle, herring sperm, sponges, and mammalian brain tissue. Agmatine is currently in the experimental and research stage. As an investigational drug, a non-blinded prospective case study in the United States is evaluating it in patients aged 18 to 75 years diagnosed with small fiber peripheral neuropathy. As of July 2013, the results of this study have not been published. As an experimental drug, arginine is being investigated for the treatment of various diseases, such as cardioprotection, diabetes, decreased renal function, neuroprotection (stroke, severe central nervous system injury, epilepsy, glaucoma, and neuropathic pain), and mental illnesses (depression, anxiety, schizophrenia, and cognitive impairment). The exact mechanism of action of arginine is still under investigation to evaluate all its potential indications. Arginine is a metabolite found in or produced by Escherichia coli (K12, MG1655 strains). It has also been reported to be present in soybeans, scallops, and other organisms with relevant data. Arginine is decarboxylated arginine and can be isolated from various plant and animal sources, such as pollen, ergot, herring sperm, and octopus muscle. Drug Indications Experimental studies are currently underway to evaluate the application of arginine in various indications, such as cardioprotection, diabetes, renal impairment, neuroprotection (stroke, severe central nervous system injury, epilepsy, glaucoma, and neuropathic pain), and mental illnesses (depression, anxiety, schizophrenia, and cognitive impairment). As an investigational drug, Agmatine is undergoing a non-blinded prospective case study in the United States in patients diagnosed with small fiber peripheral neuropathy. Mechanism of Action The exact mechanism of action for all potential indications of Agmatine is still under investigation. Several biochemical mechanisms have been identified that are related to the indications of Agmatine in diabetes, neuroprotection, and mental illness. In diabetes, Agmatine increases cellular glucose uptake by increasing insulin release from pancreatic islet cells and by increasing adrenal endorphin release, thus producing a hypoglycemic effect. In neuroprotection, the effects of Agmatine are thought to involve the regulation of receptors (NMDA, α2, and imidazoline receptors) and ion channels (ATP-sensitive potassium channels and voltage-gated calcium channels), as well as blocking nitric oxide synthesis. Arginine blocks nitric oxide synthesis by reducing the protein levels of nitric oxide synthase-2 (NOS-2) in astrocytes and macrophages. Regarding the therapeutic effects of arginine in mental illness, studies suggest that its mechanism involves the regulation of neurotransmitter receptors, including NMDA receptors, α2 receptors, serotonin receptors, opioid receptors, and imidazoline receptors. Specifically, when arginine binds to imidazoline and α2 receptors, it acts as a neurotransmitter, prompting the adrenal glands to release catecholamines.

C5H14N4

130.122

306-60-5

306-60-5 ( free base);2482-00-0 (sulfate);

199

Typically exists as solid at room temperature

1.2 g/cm3

281.4ºC at 760 mmHg

234-238 degress Celcius

124ºC

1.099

3

2

4

9

85

0

NCCCCNC(N)=N

QYPPJABKJHAVHS-UHFFFAOYSA-N

InChI=1S/C5H14N4/c6-3-1-2-4-9-5(7)8/h1-4,6H2,(H4,7,8,9)

2-(4-aminobutyl)guanidine

NSC56332NSC 56332Agmatine NSC-56332

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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 Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

---

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
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

---

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

---

 (Please use freshly prepared in vivo formulations for optimal results.)