Agmatine sulfate

Catalog No.S4962

For research use only.

Agmatine sulfate is a bioactive metabolite of the arginine amino acid. It has been shown to increase nitric oxide, reduce blood sugar levels and even increase growth hormone levels.

Agmatine sulfate Chemical Structure

CAS No. 2482-00-0

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Biological Activity

Description Agmatine sulfate is a bioactive metabolite of the arginine amino acid. It has been shown to increase nitric oxide, reduce blood sugar levels and even increase growth hormone levels.
iNOS [4]
In vitro

Agmatine has been reported to act as a ligand of the imidazoline receptor. It inhibits all isoforms of nitric oxide synthase (NOS) and blocks nicotinic receptor, voltage-gated Ca2+ channels and N-methyl-d-aspartate (NMDA) receptor channels. Agmatine could prevent neurotoxicity produced by glutamate in cultured cerebellar granule cells[1]. Agmatine acts as an antiproliferative agent in several non-intestinal mammalian cell models. It markedly accumulates inside the cells without being metabolised and exerts a strong cytostatic effect with an IC50 close to 2 mM in human colon adenocarcinoma HT-29 Glc−/+ cell line. Agmatine interferes with both polyamine metabolism and DNA synthesis resulting in alterations in the cell cycle and cell growth: it induces the accumulation of cells in the S and G2/M phases, reduces the rate of DNA synthesis and decreases cyclin A and B1 expression[2].

In vivo Agmatine exerts its neuroprotective action by reducing the size of ischemic infarctions or the loss of cerebellar neurons after focal or global ischemia in vivo. Its neuroprotective effects also include attenuating the extent of neuronal loss following excitotoxic spinal cord injury[1]. In mammalian brain, agmatine is an endogenous neurotransmitter and/or neuromodulator. Agmatine is an endogenous ligand at imidazoline receptors, to which it binds with high affinity. It exerts a significant anxiolytic effect in both rats and mice. When exogenously administered to rodents, agmatine decreases the hyperalgesia accompanying inflammation, normalizes the mechanical hypersensitivity (allodynia/hyperalgesia) produced by chemical or mechanical nerve injury, and reduces autotomy-like behavior and lesion size after excitotoxic spinal cord injury. Agmatine also exerts a notable antidepressant effect in animal models, which is related to its inhibition of N-methyl-d-aspartate (NMDA) receptors. Peripheral injection of agmatine can cross the blood-brain barrier[3]. agmatine has hepatoprotective effects against GalN/LPS-induced Fulminant hepatic failure (FHF) in mice that may be related to its ability to suppress oxidative stress, NO synthesis and TNF-α production[4].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: human colon adenocarcinoma HT-29 Glc−/+ cell line
  • Concentrations: 1-5 mM
  • Incubation Time: 0-12 days
  • Method: Cells are grown at 37℃ under 10% CO2 atmosphere in a Dulbecco modified Eagle medium (DMEM) containing 4 mM l-glutamine, 25 mM d-glucose and supplemented with 10% fetal calf serum (FCS). HT-29 Glc−/+ cells are used from passage 40 to 71 (1 passage per week). Agmatine sulfate or equal amounts of H2SO4 (control) is always added 2 days after cell seeding in DMEM supplemented with 3% horse serum (HS) in order to avoid the polyamine degradation by serum amine and diamine oxidase (DAO) activities. Cells are seeded at a density of 5×103 cells per well on 96-well tissue culture microplates and cell proliferation is determined using the method of DNA fluorometric assay using bis-benzimide trihydrochloride i.e. Hoechst 33342.
Animal Research:[3]
  • Animal Models: Male Kun-ming strain mice
  • Dosages: 20-80 mg/kg, s.c or 10-40 mg/kg, p.o
  • Administration: p.o. or s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 228.27


CAS No. 2482-00-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C(CCN=C(N)N)CN.OS(=O)(=O)O

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